US2007148185A1PendingUtilityA1
Novel therapeutic target for protozoal diseases
Est. expiryOct 14, 2025(expired)· nominal 20-yr term from priority
A61K 39/00C07K 14/445A61K 2039/505G01N 33/56905Y02A50/30A61K 2039/522G01N 2333/445A61K 2039/53
50
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
A novel Hemozoin Detoxification Protein (HDP) from Plasmodium and related parasites is provided as a target for therapeutic intervention in diseases caused by the parasites. HDP has been shown to play a critical role in adhesion to, or invasion into, host cells by the parasite. Furthermore, HDP catalyzes the neutralization of heme by the parasite, by promoting its polymerization into hemozoin. This invention provides methods and compositions for therapies based on the administration of protein, DNA or cell-based vaccines and/or antibodies based on HDP, or antigenic epitopes of HDP, either alone or in combination with other parasite antigens. Methods for the development and use of compounds that inhibit the catalytic activity of HDP, and diagnostic and laboratory methods utilizing HDP are also provided. HDP is also referred to herein as Fasciclin Related Adhesive Protein (FRAP).
Claims
exact text as granted — not AI-modified1 . A method of treating or preventing a disease caused by a Plasmodium or Theileria parasite in an individual in need thereof, comprising the step of
inhibiting interaction of heme and Heme Detoxification Protein (HDP) in said individual.
2 . The method of claim 1 , wherein said step of inhibiting is carried out by administering to said individual one or more compounds that inhibit interaction of heme and HDP.
3 . The method of claim 2 , wherein said one or more compounds bind to heme.
4 . The method of claim 3 , wherein said one or more compounds prevent heme from binding to HDP.
5 . The method of claim 3 , wherein said one or more compounds allow the binding of heme to HDP but prevent detoxification of heme by HDP.
6 . The method of claim 2 , wherein said one or more compounds bind to HDP.
7 . The method of claim 6 , wherein said one or more compounds prevent binding of heme to HDP.
8 . The method of claim 6 , wherein said one or more compounds prevent the production of hemozoin from bound heme.
9 . The method of claim 6 , wherein said one or more compounds bind at the active site of HDP.
10 . The method of claim 6 , wherein said one or more compounds bind at an allosteric site of HDP.
11 . The method of claim 1 , wherein said step of inhibiting is carried out by modification of a cell membrane of said Plasmodium or Theileria parasite.
12 . The method of claim 1 , wherein said step of inhibiting is carried out by inhibiting secretion of HDP from said Plasmodium or Theileria parasite.
13 . The method of claim 2 wherein said disease is malaria.
14 . The method of claim 13 , wherein said compound is administered to said individual in combination with one or more of: an additional antimalarial agent, an agent for reversing antimalarial resistance, and an adjuvant.
15 . The method of claim 14 , wherein said compound is administered prior to, concurrent with, or subsequent to administration of said additional antimalarial agent or said agent for reversing antimalarial resistance.
16 . The method of claim 14 , wherein said additional antimalarial agent is selected from the group consisting of a) quinolines, b) folic acid antagonists, c) sulfonamides, and d) antibiotics.
17 . The method of claim 14 , wherein said agent for reversing antimalarial resistance is an inhibitor of multidrug resistance.
18 . The method of claim 2 , wherein said compound is administered orally, parenterally, sublingually, rectally, topically or with an inhalation spray.
19 . The method of claim 2 wherein said one or more compounds is selected from the group consisting of:
(1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)-3-(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1H-perimidine-2-carboxylic acid; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl}-1H-isoindole-1,3(2H)-dione; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-[(4-{[(2R)-tetrahydrofuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl}oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimethylaniline; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5-7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chromen-4-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-chloro-N-[2-(dimethylamino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; N-(2-ethoxyphenyl)-2-hydroxybenzamide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diamine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; and O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O)c(O)c4)O [C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1═O)c26)[C@@H]3OC (═O)c7cc(O)c(O)c(O)c7.
20 . The method of claim 2 wherein said one or more compounds is selected from the group consisting of:
(10S)-10-(dimethylamino)-9-methyl-7H,10H-naphtho[1,8-gh]chromen-7-one; (1E,4E)-1-[4-(dimethylamino)phenyl]-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one; (1R,3R)-1-isopropyl-2,3,4,9-tetrahydro-1H-beta-carboline-3-carboxylic acid; (1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E)-3-(3,4-dimethoxyphenyl)-N-(3,4-dimethylphenyl)acrylamide; (2E)-6-ethoxy-2-(2-hydroxybenzylidene)-1-benzothiophen-3(2H)-one; (2E)-N-(2-methyl-1,3-benzothiazol-6-yl)-3-phenylacrylamide; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2E,5Z)-2-[(2-chlorophenyl)imino]-5-(4-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (2R)-1-(benzylamino)-3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol; (2R)-2-(2,4-dichlorophenoxy)-N-(5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)propanamide; (2R)-2-[(5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid; (2R)-2-[(E)-2-(1,3-benzodioxol-5-yl)vinyl]-5,6-dimethyl-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-one; (2R,3Z)-6-chloro-3-[(dimethylamino)methylene]-2-methyl-2,3-dihydro-4H-thiochromen-4-one; (2S)-2-(4-chlorophenyl)-3-oxo-4-phenylbutanenitrile; (2S)-2-[(5E)-5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]succinic acid; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (2S,3Z)-3-(1H-indol-3-ylmethylene)-2-phenyl-2,3-dihydro-4H-chromen-4-one; (2Z)-2-acetamido-N-(3,5-dimethylphenyl)-3-phenylacrylamide; (2Z,5E)-2-[(3,5-dimethylphenyl)imino]-5-(2-hydroxy-3-methoxybenzylidene)-1,3-thiazolidin-4-one; (2Z,5Z)-2-[(2-chlorophenyl)imino]-5-(2-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (3,5-dichloro-2-hydroxyphenyl)(isoxazol-4-yl)methanone; (3-{(E)-[1-(3-fluorophenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl}-1H-indol-1-yl)acetonitrile; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3aS,6aS)-3-benzoyl-1,5-diphenyl-3a,6a-dihydropyrrolo[3,4-c]pyrazole-4,6(1H,5H)-dione; (3R)-3-(2-hydroxy-4-methylphenyl)-N-(2-methoxyphenyl)-3-phenylpropanamide; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; (3R,3′R,4′S,6′R,8′S,8a′S)-5-(4-hydroxybut-1-yn-1-yl)-6′-[4-(2-hydroxyethoxy)phenyl]-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2, 1-c][1,4]oxazine]-8′-carboxylic acid; (3S)-3-(2-hydroxy-4-methylbenzoyl)-2-(4-methylphenyl)isoindolin-1-one; (3S,3aR,6aR)-3-(5-bromo-2-hydroxyphenyl)-5-butyl-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazole-4,6(3H,5H)-dione; (3S,6S,7R,8aR)-3-(4-acetamidobutyl)-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazine-7-carboxylic acid; (3Z)-3-(3-hydroxy-4-methoxybenzylidene)-1-methyl-1,3-dihydro-2H-indol-2-one; (4E)-2-(4-methoxyphenyl)-4-[(4-methoxyphenyl)imino]-4H-chromen-6-ol; (4R)-3-(3,4-dichlorophenyl)-4-hydroxy-N-isopropyl-2-oxo-1,2,3,4-tetrahydroquinazoline-4-carboxamide; (4R)-4-(4-bromophenyl)-3-hydroxy-1-isopropyl-4,8-dihydro-1H-pyrazolo[3,4-e][1,4]thiazepin-7(6H)-one; (4R)-4-(4-ethylphenyl)-3-hydroxy-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4R)-5-(2-furylmethyl)-3-(2-hydroxyphenyl)-4-phenyl-4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-one; (4R)-N˜4˜-(6-chloro-2-methoxyacridin-9-yl)-N˜1˜,N˜1˜-diethylpentane-1,4-diamine; (4S)-4-(2-bromobenzoyl)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one; (4S)-4-(2-furyl)-3-hydroxy-7,7-dimethyl-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4S)-5,7-dihydroxy-4-phenylchroman-2-one; (4S,5S)-3,5-diphenyl-4,5-dihydro-1H-pyrazol-4-ol; (4S,7R)-2-amino-4-isobutyl-5-oxo-7-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile; (4Z)-2-[2-(4-chlorophenoxy)pyridin-3-yl]-4-[(dimethylamino)methylene]-1,3-oxazol-5(4H)-one; (5E)-1-(4-methylpentyl)-5-(1H-pyrrol-2-ylmethylene)pyrimidine-2,4,6(1H,3H,5H)-trione; (5E)-3-allyl-5-(2-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one; (5E)-5-[4-(diethylamino)benzylidene]-3-{[(2-methoxyphenyl)amino]methyl}-1,3-thiazolidine-2,4-dione; (5R)-5-methyl-4-phenyl-1,3,4-thiadiazolidine-2-thione; (5S,7R)-2,2-dimethyl-5,7-bis(2-phenylethyl)-7,8-dihydro-4H,5H-pyrano[4,3-d][1,3]dioxine; (5Z)-5-(4-hydroxybenzylidene)-3-[(2R)-tetrahydrofuran-2-ylmethyl]-2-thioxo-1,3-thiazolidin-4-one; (6E)-5-imino-6-{[1-(2-naphthyl)-1H-pyrrol-2-yl]methylene}-5,6-dihydro-7H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one; *c1ceccc1C2C(═O)N(C)c3ccccc3C2=O; [(2R)-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]acetic acid; [(5E)-4-oxo-5-(3-thienylmethylene)-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [(5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; {4-[(4-methylphenyl)sulfonyl]phenyl}hydrazine; 1-(2,4-dihydroxy-6-methylphenyl)-2-phenoxyethanone; 1-(2,4-dihydroxyphenyl)-2-(4-isopropylphenoxy)ethanone; 1-(3,4-dihydroxyphenyl)-2-({4-[(3,5-dimethoxyphenyl)amino]quinazolin-2-yl}thio)ethanone; 1-(4-chlorophenyl)-1-hydroxy-3-phenylurea; 1-(4-hydroxy-3,5-dimethylphenyl)-2-[(4-methylphenyl)thio]ethanone; 1-(4-iodo-2-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-ol; 1-(5-butyl-2,4-dihydroxyphenyl)-2-pyridin-2-ylethanone; 1-(5-ethyl-2,4-dihydroxyphenyl)-2-(1-methyl-1H-benzimidazol-2-yl)ethanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)- 3 -(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-[4-(7-chloroquinolin-4-yl)piperazino]propan-1-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1-ethynyl-2-phenoxybenzene; 1H-perimidine-2-carboxylic acid; 2-(1,3-benzodioxol-5-yl)-1-(2,4-dihydroxy-5-propylphenyl)ethanone; 2-(1H-benzimidazol-1-yl)-1-(5-ethyl-2,4-dihydroxyphenyl)ethanone; 2-(2,4-dichlorophenyl)-1H-imidazo[4,5-b]pyridin-1-ol; 2-(2,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,5-dihydroxy-7-methoxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-chlorophenyl)-4H-1,3-benzoxazin-4-one; 2-(4-chlorophenyl)-5-{[(4-pyridin-3-ylpyrimidin-2-yl)thio]methyl}-2,4-dihydro-3H-pyrazol-3-one; 2-(4-fluoro-3-phenoxyphenyl)-3-hydroxy-4H-chromen-4-one; 2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)-N-(4-methylphenyl)acetamide; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(4-methylphenyl)-4H-1,3-benzoxazin-4-one; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2,2′-thiobis(4-chlorophenol); 2,4-dichloro-1-naphthyl[2,2,2-trifluoro-1-methyl-1-(trifluoromethyl)ethyl]carbamate; 2-[(2-phenoxyethyl)thio]quinazoline-4-thiol; 2-[(2R)-6,7-dimethyl-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]-N-ethylacetamide; 2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]-N-1-naphthylacetamide; 2-[(5S)-1-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-5-yl]phenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]phenol; 2-[5-(ethylsulfonyl)-2-hydroxyphenyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione; 2-{(1R)-1-[(1-allyl-1H-benzimidazol-2-yl)amino]ethyl}-4-chlorophenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl}-1H-isoindole-1,3(2H)-dione; 2-{[5-chloro-6-methyl-2-(2-pyridinyl)-4-pyrimidinyl]sulfanyl}-1-phenyl-1-ethanone; 2-amino-1-(2,4-dimethylphenyl)-1H-pyrrolo[2,3-b]quinoxaline-3-carbonitrile; 2-amino-5-butyl-4-(4-hydroxy-3-methoxyphenyl)-6-phenylnicotinonitrile; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-anilino-2-oxoethyl 2-(4-chlorobenzoyl)benzoate; 2-chloro-5-phenyl-3-pyridin-4-yl-4H-1,4-thiazine; 2-chloro-8-hydroxy-10,10-dimethyl-7-phenylpyrido[1,2-a]indol-6(10H)-one; 2-hydrazino-4,6-diphenylpyrimidine; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-methylphenyl)benzamide; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 2-hydroxy-N-[(4-methyl-2-phenyl-1,3-thiazol-5-yl)carbonyl]benzamide; 2-hydroxy-N-[2-(2-methoxyphenyl)acetyl]benzamide; 2-hydroxy-N-{[2-(4-methylphenoxy)-3-pyridinyl]carbonyl}benzamide; 2-hydroxy-N-pyridin-3-ylbenzamide; 2-phenyl-4H-thiochromene-4-thione; 2-phenyl-5-({[5-(trifluoromethyl)pyridin-2-yl]sulfonyl}methyl)-2,4-dihydro-3H-pyrazol-3-one; 2-phenyl-5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3-one; 3-(1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)-N-(2-hydroxyphenyl)-N-(4-methoxybenzyl)propanamide; 3-(1-acetyl-1H-indol-3-yl)-4-hydroxy-2H-chromen-2-one; 3-(1H-benzimidazol-1-yl)-6-ethyl-7-hydroxy-4H-chromen-4-one; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(3-{[(4-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(4-bromophenyl)-7-hydroxy-2-methyl-4H-chromen-4-one; 3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)propan-1-one; 3-(5-{(Z)-[5-(4-methylphenyl)-2-oxofuran-3(2H)-ylidene]methyl}-2-furyl)benzoic acid; 3-(quinazolin-4-ylamino)phenyl thiophene-2-carboxylate; 3,4-dimethoxy-N-(4-methyl-1,3-benzothiazol-2-yl)benzamide; 3,5-dichloro-2-hydroxybenzaldehyde N-tert-butyl-N′-methylthiosemicarbazone; 3-[(4-{[(2R)-tetrahydrofuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[2-(4-methoxyphenyl)ethyl]-10-methyl-6-phenyl-3,4-dihydro-2H,8H-chromeno[6,7-e][1,3]oxazin-8-one; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 3-{2-[(1,3-dioxo-1,3-dihydro-2H-inden-2-ylidene)methyl]-1H-pyrrol-1-yl}benzoic acid; 3-benzyl-4-hydroxy-1,2-dihydroquinolin-2-one; 3-benzyl-4-hydroxy-1-phenylquinolin-2(1H)-one; 3-benzyl-5,6-bis(4-methoxyphenyl)furo[2,3-d]pyrimidin-4(3H)-imine; 3-benzyl-5-ethyl-4-hydroxy-6-phenyl-1-(1,3-thiazol-2-yl)pyridin-2(1H)-one; 3-benzyl-6-ethoxy-4-hydroxyquinolin-2(1H)-one; 3-chloro-N-[2-(methylthio)-1,3-benzothiazol-6-yl]benzamide; 3-hydroxy-N-(2-methylphenyl)-2-naphthamide; 3-methoxy-2-methyl-6-[1′-phenyl-5-(trifluoromethyl)-1H, 1′H-4,4′-bipyrazol-3-yl]phenol; 3-methoxy-N-(3-[1,3]oxazolo[4,5-b]pyridin-2-ylphenyl)benzamide; 3-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-5-ol; 3-methyl-1-phenyl-4-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[3,4-b]pyridin-6-one; 3-methyl-4-[(4-methylphenyl)thio]-1-phenyl-1H-pyrazol-5-yl methoxyacetate; 3-oxo-3-[3-({[3-(trifluoromethyl)phenyl]thio}methyl)phenyl]propanenitrile; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl}oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimethylaniline; 4-(1-propyl-1H-benzimidazol-2-yl)aniline; 4-(2,6-dichlorobenzyl)-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-[(2,3,5,6-tetrafluoro-1,4-phenylene)bis(oxy)]diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(3S,6S,7R,8aR)-7-{[2-(4-{(3S,3′S,4′R,6′R,8′R,8a′R)-8′-[(allyloxy)carbonyl]-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2, 1-c][1,4]oxazin]-6′-yl}phenoxy)ethoxy]carbonyl}-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-3-yl]-N,N,N-trimethylbutan-1-aminium; 4-[(4-chlorophenyl)thio]-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[1-(4-hydroxy-3-methoxybenzyl)-1H-benzimidazol-2-yl]-2-methoxyphenol; 4-[1′-phenyl-5-(trifluoromethyl)-1H,1′H-4,4′-bipyrazol-3-yl]benzene-1,3-diol; 4-[4-(1,3-benzothiazol-2-yl)-5-methyl-1H-pyrazol-3-yl]benzene-1,3-diol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]-1-methyl-1H-pyrazol-5-amine; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(1E)-3-(2-furyl)-3-oxoprop-1-en-1-yl]amino}benzoic acid; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-{[(2S)-2-ethylpiperidin-1-yl]methyl}-3-hydroxy-1-methyl-6H-benzo[c]chromen-6-one; 4-bromo-2-[(E)-(4H-1,2,4-triazol-4-ylimino)methyl]phenol; 4-bromo-2-[5-(2-furyl)-1H-pyrazol-3-yl]phenol; 4-bromo-6-chloro-2-oxo-1,3-benzoxathiol-5-yl ethyl carbonate; 4-ethyl-6-[4-(1-methyl-1H-benzimidazol-2-yl)-1H-pyrazol-3-yl]benzene-1,3-diol; 4-fluoro-N-[3-(trifluoromethyl)phenyl]benzamide; 4-hydroxy-3-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-2H-chromen-2-one; 4-hydroxy-3-propylquinolin-2(1H)-one; 4-hydroxy-5-phenyl-6H-pyrido[3,2,1-jk]carbazol-6-one; 4-hydroxy-8-methyl-3-{(E)-[(3R)-5-oxo-1,3-diphenylpyrazolidin-4-ylidene]methyl}quinolin -2(1H)-one; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-bromo-2-hydroxybenzoyl)-1-(2-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5-(benzoylamino)-N,N′-bis(2-hydroxyphenyl)isophthalamide; 5-(diethylamino)-2-{(E)-[(2-phenylethyl)imino]methyl}phenol; 5,7-dihydroxy-4-propyl-2H-chromen-2-one; 5-[(4-methylphenyl)thio]quinazoline-2,4-diamine; 5-{2-[(3,4-dichlorophenyl)thio]ethyl}-2-methylpyridine; 5-benzyl-3-phenyl-5H-pyrazolo[4,3-c]quinolines; 5-benzyl-4-hydroxy-6H-pyrido[3,2,1-jk]carbazol-6-one; 5-chloro-2-hydroxy-N-phenylbenzamide; 5-hydroxy-4-methyl-7-propyl-2H-chromen-2-one; 5-methoxy-2-[3-methyl-4-(1,3-thiazol-4-yl)isoxazol-5-yl]phenol; 5-methyl-2-[5-(2-thienyl)-1H-pyrazol-3-yl]phenol; 6-(4-chlorophenyl)-7-hydroxy-1,3-dimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione″6,6′-biquinoline; 6-[(S)-[4-(dimethylamino)phenyl](piperidin-1-yl)methyl]-1,3-benzodioxol-5-ol; 6-{[(2-ethylphenyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-{[(4-chlorophenyl)thio]methyl}-2-phenyl-1H-pyrazolo[3,4-b]pyridine-3,4(2H,7H) -dione; 6-{[(4-ethoxyphenyl)(methyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-allyl-7-hydroxy-4,8-dimethyl-2H-chromen-2-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-benzyl-7-hydroxy-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one; 6-bromo-2-(trifluoromethyl)quinolin-4-ol; 6-butyl-2-(2-furyl)-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidin-7-one; 6-chloro-2-(4-chlorophenyl)-1H-benzimidazol-1-ol; 6-chloro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-chloro-3-(4-methylphenyl)-3,4-dihydro-2H-1,3-benzoxazine; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 6-ethyl-7-hydroxy-3-(1-methyl-1H-benzimidazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 6-fluoro-4-hydroxy-3-phenylquinolin-2(1H)-one; 6-methoxy-N-[(1S)-1-methylpropyl]furo[2,3-b]quinoline-2-carboxamide; 6-phenyl[1,2,3,4]tetraazolo[1,5-b]pyridazin-7-ol; 7-(4-bromophenyl)-5-hydroxy-1,3-benzoxathiol-2-one; 7,8-dihydroxy-2-phenyl-4H-chromen-4-one; 7,8-dihydroxy-4-phenyl-2H-chromen-2-one; 7-[(2E)-2-(4-fluoro-3-phenoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[2-chloro-5-(trifluoromethyl)phenyl]-5-hydroxy-1,3-benzoxathiol-2-one; 7-{(2E)-2-[(2-fluorobiphenyl-4-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-benzyl-8-hydroxy-10,10-dimethyl-6,10-dihydropyrido[1,2-a]indol-6-one; 7-chloro-4-piperidinoquinoline; 7-chloro-N-(3-fluoro-4-methylphenyl)quinolin-4-amine; 7-chloro-N-[2-(dimethylamino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 7-hydroxy-5-methyl-3-(1-phenyl-1H-pyrazol-4-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 7-hydroxy-6-methyl-3-(4-methyl-1,3-thiazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 8-(trifluoromethoxy)-2-(trifluoromethyl)quinolin-4-ol; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-[(2E)-2-(5-bromo-2-methoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-{(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-methoxy-N,N-dimethyl-5H-pyrimido[5,4-b]indol-4-amine; allyl(3R,3′R,4′S,6′R,8′S,8a′S)-6′-{4-[2-({[(3S,6R,7S,8aS)-3-[4-(dimethylamino)butyl]-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-7-yl]carbonyl}oxy)ethoxy]phenyl}-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2,1-c][1,4]oxazine]-8′-carboxylate” bis[4-(dimethylamino)phenyl]methanone oxime; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COC(═O)[C@]1(Cc2ccc(O)c(CC═C(C)C)c2)OC(═O)C(═C1c3ccc(O)cc3)O; COc1cc(/C═C/2\Oc3cc(O)ccc3C2=O)ccc1O; COc1cc(ccc1O)c2oc3cc(O)cc(O)c3c(═O)c2O; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl(2E)-3-(2-hydroxy-5-nitrophenyl)acrylate; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; ethyl 4-(benzylamino)-6-ethoxyquinoline-3-carboxylate; ethyl 4-[({[(5R)-5-ethyl-4,6-dioxo-1,4,5,6-tetrahydropyrimidin-2-yl]thio}acetyl)amino]benzoate; ethyl 4-[(2-phenylethyl)amino]quinoline-3-carboxylate; ethyl 4-{[(2-anilino-2-oxoethyl)thio]methyl}-5-hydroxy-2-phenyl-1-benzofuran-3-carboxylate; ethyl 4-{[(2E)-3-(2-thienyl)prop-2-enoyl]amino}benzoate; ethyl 6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-{[(4-methylphenyl)thio]methyl}-1H-indole-3-carboxylate; ethyl 6-ethoxy-4-{[(1R)-1-methylpropyl]amino}quinoline-3-carboxylate; ethyl 6-methyl-4-[(4-morpholin-4-ylphenyl)amino]quinoline-3-carboxylate; isopropyl (2S)-2-{[(2S)-2-{[(2S,3R)-2-{[(2S)-2-amino-3-mercaptopropyl]amino}-3-methylpentyl]oxy}-3-phenylpropanoyl]amino}-4-(methylsulfonyl)butanoate; methyl(2Z)-2-(4-hydroxybenzylidene)-3-oxo-2,3-dihydro-1-benzofuran-5-carboxylate; methyl 1-hydroxy-3-methylpyrido[1,2-a]benzimidazole-4-carboxylate; methyl 2,3-bis-O-(biphenyl-2-ylcarbamoyl)-4-O-[(3-ethylphenyl)carbamoyl]-alpha-L-idopyranoside; methyl 5-hydroxy-1-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylate; N-(1,3-benzodioxol-5-yl)-7-chloroquinolin-4-amine; N-(2,3-dihydro-1-benzofuran-5-ylcarbonyl)-2-hydroxybenzamide; N-(2,5-dimethylphenyl)benzamide; N-(2-chlorobenzyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(2-chlorobenzyl)-2-phenyl-1H-benzimidazole-5-sulfonamide; N-(2-ethoxyphenyl)-2-hydroxybenzamide; N-(2-hydroxy-4-methylphenyl)-4-[(methylthio)methyl]benzamide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(2-hydroxybenzoyl)-4-(trifluoromethyl)benzamide; N-(2-hydroxyphenyl)-8-[(2E)-2-(1-naphthylmethylene)hydrazino]-8-oxooctanamide; N-(3-bromo-4-hydroxy-1-naphthyl)-4-chlorobenzenesulfonamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-chlorophenyl)-4-(5-hydroxy-1-phenyl-1H-pyrazol-3-yl)piperidine-1-carbothioamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(3-hydroxypyridin-2-yl)-4-phenoxybenzamide; N-(3-imidazo[1,2-a]pyrimidin-2-ylphenyl)cyclopentanecarboxamide; N-(4-bromophenyl)-2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]acetamide; N-(4-carbamoylphenyl)-1-phenyl-3-(2-thienyl)-1H-pyrazole-4-carboxamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(4-fluorophenyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(5-{[(1S)-1-methylpropyl]thio}-1,3,4-thiadiazol-2-yl)-2-(trifluoromethyl)benzamide; N-(5-hydroxy-1-naphthyl)-4-methylbenzenesulfonamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-(6-methyl-1,3-benzothiazol-2(3H)-ylidene)thiophene-2-carboxamide; N-(cyclohexylcarbonyl)-2-hydroxybenzamide; N,2-diphenylquinazolin-4-amine; N,N,8-trimethyl-5H-pyrimido[5,4-b]indol-4-amine; N,N′-1H-isoindole-1,3(2H)-diylidenedianiline; N,N-diethyl-8-methyl-5H-pyrimido[5,4-b]indol-4-amine; N,N-dimethyl-4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzenesulfonamide; N-[(1E)-(9-ethyl-9H-carbazol-3-yl)methylene]-4H-1,2,4-triazol-4-amine; N-[(1E)-1H-indol-3-ylmethylene]-1-propyl-1H-benzimidazol-2-amine; N-[(1S)-1-benzylpropyl]-6-[(4-methylpiperidin-1-yl)sulfonyl]-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(3-chloro-1-benzothiophen-2-yl)carbonyl]-2-hydroxybenzamide; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N-[2-(1H-benzimidazol-2-yl)phenyl]-2-methylpropanamide; N-[2-chloro-5-(trifluoromethyl)phenyl]-2-(4,4-dimethyl-2,6-dioxocyclohexyl)acetamide; N-[2-hydroxy-3-(4-oxo-4H-chromen-2-yl)phenyl]acetamide; N-[3-(1,3-benzothiazol-2-yl)-4-hydroxyphenyl]-2,2-dimethylpropanamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]benzenesulfonamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]thiophene-2-sulfonamide; N-[4-(1H-benzimidazol-2-yl)phenyl]-2-(2-methoxyphenyl)acetamide; N-[4-(ethylsulfonyl)-2-hydroxyphenyl]benzamide; N-[5-(ethylsulfonyl)-2-hydroxyphenyl]-2-(4-methoxyphenoxy)acetamide; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diamine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; N-benzyl-2-hydroxybenzamide; N-benzyl-6-{[(3-methoxyphenyl)amino]sulfonyl}-N-methyl-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)/C═C/c4ccccc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](Oc2c([C@H]3[C@@H](Oc4cc(O)cc(O)c4C3=O)c5ccc(O)cc5)c(O)cc(O)c2C1=O)c6ccc(O)cc6; O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O)c(O)c4) O[C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1=O)c26)[C@@H]3OC(═O)c7cc(O)c(O)c(O)c7; OC[C@H]1O[C@@H](OC[C@H]2O[C@@H](Oc3c(oc4cc(O)cc(O)c4c3=O)c5ccc(O)cc5)[ C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O; and OC1[C@H](OC(═O)c2cc(O)c(O)c(O)c2)OC3COC(═O)c4cc(O)c(O)c(O)c4-c5c(O)c(O)c(O)cc5C(═O)O[C@@H]1[C@@H]3OC(═O)c6cc(O)c(O)c(O)c6c7c(O)c(O)c(O)cc7C(═O)OOc1ccc(cc1)[C@H]2CC(═O)c3c(O)cc(O)c([C@H]4[C@@H](Oc5cc(O)cc(O)c5C4=O)c6ccc(O)cc6) c3O2Oc1ccc2C(═O)/C(═C/c3ccc(O)c(O)c3)/Oc2c1.
21 . A method of inhibiting heme detoxification in a Plasmodium or Theileria parasite, comprising the step of
preventing or attenuating the production of hemozoin by HDP in said Plasmodium or Theileria parasite.
22 . The method of claim 21 wherein said step of preventing or attenuating is carried out by a process selected from the group consisting of:
1) inhibiting interaction of heme and HDP; 2) preventing an interaction of HDP or heme with cofactors; 3) preventing dimerization of HDP; and 4) preventing interaction of HDP or heme with lipids.
23 . The method of claim 22 , wherein said cofactors are selected from the group consisting of metal ions, natural ligands or protein factors.
24 . The method of claim 22 , wherein said step of preventing or attenuating is carried out by administering to said individual one or more compounds selected from the group consisting of:
(1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)-3-(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1H-perimidine-2-carboxylic acid; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl}-1H-isoindole-1,3(2H)-dione; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-[(4-{[(2R)-tetrahydrofuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl}oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimethylaniline; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chromen-4-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-chloro-N-[2-(dimethylamino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; N-(2-ethoxyphenyl)-2-hydroxybenzamide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diamine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; and O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O)c(O)c4) O[C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1=O)c26)[C@@H]3OC(═O)c7cc(O)c(O)c(O)c7.
25 . The method of claim 21 wherein said step of preventing or attenuating is carried out by administering to said individual one or more compounds selected from the group consisting of: (10S)-10-(dimethylamino)-9-methyl-7H,10H-naphtho[1,8-gh]chromen-7-one;
(1E,4E)-1-[4-(dimethylamino)phenyl]-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one; (1R,3R)-1-isopropyl-2,3,4,9-tetrahydro-1H-beta-carboline-3-carboxylic acid; (1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E)-3-(3,4-dimethoxyphenyl)-N-(3,4-dimethylphenyl)acrylamide; (2E)-6-ethoxy-2-(2-hydroxybenzylidene)-1-benzothiophen-3(2H)-one; (2E)-N-(2-methyl-1,3-benzothiazol-6-yl)-3-phenylacrylamide; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2E,5Z)-2-[(2-chlorophenyl)imino]-5-(4-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (2R)-1-(benzylamino)-3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol; (2R)-2-(2,4-dichlorophenoxy)-N-(5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)propanamide; (2R)-2-[(5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid; (2R)-2-[(E)-2-(1,3-benzodioxol-5-yl)vinyl]-5,6-dimethyl-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-one; (2R,3Z)-6-chloro-3-[(dimethylamino)methylene]-2-methyl-2,3-dihydro-4H-thiochromen-4-one; (2S)-2-(4-chlorophenyl)-3-oxo-4-phenylbutanenitrile; (2S)-2-[(5E)-5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]succinic acid; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (2S,3Z)-3-(1H-indol-3-ylmethylene)-2-phenyl-2,3-dihydro-4H-chromen-4-one; (2Z)-2-acetamido-N-(3,5-dimethylphenyl)-3-phenylacrylamide; (2Z,5E)-2-[(3,5-dimethylphenyl)imino]-5-(2-hydroxy-3-methoxybenzylidene)-1,3-thiazolidin-4-one; (2Z,5Z)-2-[(2-chlorophenyl)imino]-5-(2-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (3,5-dichloro-2-hydroxyphenyl)(isoxazol-4-yl)methanone; (3-{(E)-[1-(3-fluorophenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl}-1H-indol-1-yl)acetonitrile; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3aS,6aS)-3-benzoyl-1,5-diphenyl-3a,6a-dihydropyrrolo[3,4-c]pyrazole-4,6(1H,5H) -dione; (3R)-3-(2-hydroxy-4-methylphenyl)-N-(2-methoxyphenyl)-3-phenylpropanamide; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; (3R,3′R,4′S,6′R,8′S,8a′S)-5-(4-hydroxybut-1-yn-1-yl)-6′-[4-(2-hydroxyethoxy)phenyl]-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2,1-c][1,4]oxazine]-8′-carboxylic acid; (3S)-3-(2-hydroxy-4-methylbenzoyl)-2-(4-methylphenyl)isoindolin-1-one; (3S,3aR,6aR)-3-(5-bromo-2-hydroxyphenyl)-5-butyl-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazole-4,6(3H,5H)-dione; (3S,6S,7R,8aR)-3-(4-acetamidobutyl)-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazine-7-carboxylic acid; (3Z)-3-(3-hydroxy-4-methoxybenzylidene)-1-methyl-1,3-dihydro-2H-indol-2-one; (4E)-2-(4-methoxyphenyl)-4-[(4-methoxyphenyl)imino]-4H-chromen-6-ol; (4R)-3-(3,4-dichlorophenyl)-4-hydroxy-N-isopropyl-2-oxo-1,2,3,4-tetrahydroquinazoline-4-carboxamide; (4R)-4-(4-bromophenyl)-3-hydroxy-1-isopropyl-4,8-dihydro-1H-pyrazolo[3,4-e][1,4]thiazepin-7(6H)-one; (4R)-4-(4-ethylphenyl)-3-hydroxy-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4R)-5-(2-furylmethyl)-3-(2-hydroxyphenyl)-4-phenyl-4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H) -one; (4R)-N˜4˜-(6-chloro-2-methoxyacridin-9-yl)-N˜1˜,N˜1˜-diethylpentane-1,4-diamine; (4S)-4-(2-bromobenzoyl)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one; (4S)-4-(2-furyl)-3-hydroxy-7,7-dimethyl-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4S)-5,7-dihydroxy-4-phenylchroman-2-one; (4S,5S)-3,5-diphenyl-4,5-dihydro-1H-pyrazol-4-ol; (4S,7R)-2-amino-4-isobutyl-5-oxo-7-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile; (4Z)-2-[2-(4-chlorophenoxy)pyridin-3-yl]-4-[(dimethylamino)methylene]-1,3-oxazol-5(4H)-one; (5E)-1-(4-methylpentyl)-5-(1H-pyrrol-2-ylmethylene)pyrimidine-2,4,6(1H,3H,5H)-trione; (5E)-3-allyl-5-(2-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one; (5E)-5-[4-(diethylam-ino)benzylidene]-3-{[(2-methoxyphenyl)amino]methyl}1,3-thiazolidine-2,4-dione; (5R)-5-methyl-4-phenyl-1,3,4-thiadiazolidine-2-thione; (5S,7R)-2,2-dimethyl-5,7-bis(2-phenylethyl)-7,8-dihydro-4H,5H-pyrano[4,3-d][1,3]dioxine; (5Z)-5-(4-hydroxybenzylidene)-3-[(2R)-tetrahydrofuran-2-ylmethyl]-2-thioxo-1,3-thiazolidin-4-one; (6E)-5-imino-6-{[1-(2-naphthyl)-1H-pyrrol-2-yl]methylene}-5,6-dihydro-7H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one; *cccccc1C2C(═O)N(C)c3ccccc3C2=O; [(2R)-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]acetic acid; [(5E)-4-oxo-5-(3-thienylmethylene)-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [(5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; {4-[(4-methylphenyl)sulfonyl]phenyl}hydrazine; 1-(2,4-dihydroxy-6-methylphenyl)-2-phenoxyethanone; 1-(2,4-dihydroxyphenyl)-2-(4-isopropylphenoxy)ethanone; 1-(3,4-dihydroxyphenyl)-2-({4-[(3,5-dimethoxyphenyl)amino]quinazolin-2-yl}thio)ethanone; 1-(4-chlorophenyl)-1-hydroxy-3-phenylurea; 1-(4-hydroxy-3,5-dimethylphenyl)-2-[(4-methylphenyl)thio]ethanone; 1-(4-iodo-2-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-ol; 1-(5-butyl-2,4-dihydroxyphenyl)-2-pyridin-2-ylethanone; 1-(5-ethyl-2,4-dihydroxyphenyl)-2-(1-methyl-1H-benzimidazol-2-yl)ethanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)-3-(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-[4-(7-chloroquinolin-4-yl)piperazino]propan-1-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1-ethynyl-2-phenoxybenzene; 1H-perimidine-2-carboxylic acid; 2-(1,3-benzodioxol-5-yl)-1-(2,4-dihydroxy-5-propylphenyl)ethanone; 2-(1H-benzimidazol-1-yl)-1-(5-ethyl-2,4-dihydroxyphenyl)ethanone; 2-(2,4-dichlorophenyl)-1H-imidazo[4,5-b]pyridin-1-ol; 2-(2,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,5-dihydroxy-7-methoxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-chlorophenyl)-4H-1,3-benzoxazin-4-one; 2-(4-chlorophenyl)-5-{[(4-pyridin-3-ylpyrimidin-2-yl)thio]methyl}-2,4-dihydro-3H-pyrazol-3-one; 2-(4-fluoro-3-phenoxyphenyl)-3-hydroxy-4H-chromen-4-one; 2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)-N-(4-methylphenyl)acetamide; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(4-methylphenyl)-4H-1,3-benzoxazin-4-one; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2,2′-thiobis(4-chlorophenol); 2,4-dichloro-1-naphthyl[2,2,2-trifluoro-1-methyl-1-(trifluoromethyl)ethyl]carbamate; 2-[(2-phenoxyethyl)thio]quinazoline-4-thiol; 2-[(2R)-6,7-dimethyl-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]-N-ethylacetamide; 2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]-N-1-naphthylacetamide; 2-[(5S)-1-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-5-yl]phenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]phenol; 2-[5-(ethylsulfonyl)-2-hydroxyphenyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione; 2-{(1R)-1-[(1-allyl-1H-benzimidazol-2-yl)amino]ethyl}-4-chlorophenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl}-1H-isoindole-1,3(2H)-dione; 2-{[5-chloro-6-methyl-2-(2-pyridinyl)-4-pyrimidinyl]sulfanyl}-1-phenyl-1-ethanone; 2-amino-1-(2,4-dimethylphenyl)-1H-pyrrolo[2,3-b]quinoxaline-3-carbonitrile; 2-amino-5-butyl-4-(4-hydroxy-3-methoxyphenyl)-6-phenylnicotinonitrile; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-anilino-2-oxoethyl2-(4-chlorobenzoyl)benzoate; 2-chloro-5-phenyl-3-pyridin-4-yl-4H-1,4-thiazine; 2-chloro-8-hydroxy-10,10-dimethyl-7-phenylpyrido[1,2-a]indol-6(10H)-one; 2-hydrazino-4,6-diphenylpyrimidine; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-methylphenyl)benzamide; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 2-hydroxy-N-[(4-methyl-2-phenyl-1,3-thiazol-5-yl)carbonyl]benzamide; 2-hydroxy-N-[2-(2-methoxyphenyl)acetyl]benzamide; 2-hydroxy-N-{[2-(4-methylphenoxy)-3-pyridinyl]carbonyl}benzamide; 2-hydroxy-N-pyridin-3-ylbenzamide; 2-phenyl-4H-thiochromene-4-thione; 2-phenyl-5-({[5-(trifluoromethyl)pyridin-2-yl]sulfonyl}methyl)-2,4-dihydro-3H-pyrazol-3-one; 2-phenyl-5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3-one; 3-(1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)-N-(2-hydroxyphenyl)-N-(4-methoxybenzyl)propanamide; 3-(1-acetyl-1H-indol-3-yl)-4-hydroxy-2H-chromen-2-one; 3-(1H-benzimidazol-1-yl)-6-ethyl-7-hydroxy-4H-chromen-4-one; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(3-{[(4-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(4-bromophenyl)-7-hydroxy-2-methyl-4H-chromen-4-one; 3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)propan-1-one; 3-(5-{(Z)-[5-(4-methylphenyl)-2-oxofuran-3(2H)-ylidene]methyl}-2-furyl)benzoic acid; 3-(quinazolin-4-ylamino)phenyl thiophene-2-carboxylate; 3,4-dimethoxy-N-(4-methyl-1,3-benzothiazol-2-yl)benzamide; 3,5-dichloro-2-hydroxybenzaldehyde N-tert-butyl-N′-methylthiosemicarbazone; 3-[(4-{[(2R)-tetrahydrofuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[2-(4-methoxyphenyl)ethyl]-10-methyl-6-phenyl-3,4-dihydro-2H,8H-chromeno[6,7-e][1,3]oxazin-8-one; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 3-{2-[(1,3-dioxo-1,3-dihydro-2H-inden-2-ylidene)methyl]-1H-pyrrol-1-yl}benzoic acid; 3-benzyl-4-hydroxy-1,2-dihydroquinolin-2-one; 3-benzyl-4-hydroxy-1-phenylquinolin-2(1H)-one; 3-benzyl-5,6-bis(4-methoxyphenyl)furo[2,3-d]pyrimidin-4(3H)-imine; 3-benzyl-5-ethyl-4-hydroxy-6-phenyl-1-(1,3-thiazol-2-yl)pyridin-2(1H)-one; 3-benzyl-6-ethoxy-4-hydroxyquinolin-2(1H)-one; 3-chloro-N-[2-(methylthio)-1,3-benzothiazol-6-yl]benzamide; 3-hydroxy-N-(2-methylphenyl)-2-naphthamide; 3-methoxy-2-methyl-6-[1′-phenyl-5-(trifluoromethyl)-1H,1′H-4,4′-bipyrazol-3-yl]phenol; 3-methoxy-N-(3-[1,3]oxazolo[4,5-b]pyridin-2-ylphenyl)benzamide; 3-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-5-ol; 3-methyl-1-phenyl-4-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[3,4-b]pyridin-6-one; 3-methyl-4-[(4-methylphenyl)thio]-1-phenyl-1H-pyrazol-5-yl methoxyacetate; 3-oxo-3-[3-({[3-(trifluoromethyl)phenyl]thio}methyl)phenyl]propanenitrile; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl}oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimethylaniline; 4-(1-propyl-1H-benzimidazol-2-yl)aniline; 4-(2,6-dichlorobenzyl)-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-[(2,3,5,6-tetrafluoro-1,4-phenylene)bis(oxy)]diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(3S,6S,7R,8aR)-7-{[2-(4-{(3S,3′S,4′R,6′R,8′R,8a′R)-8′-[(allyloxy)carbonyl]-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2, 1-c][1,4]oxazin]-6′-yl}phenoxy)ethoxy]carbonyl}-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-3-yl]-N,N,N-trimethylbutan-1-aminium; 4-[(4-chlorophenyl)thio]-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[1-(4-hydroxy-3-methoxybenzyl)-1H-benzimidazol-2-yl]-2-methoxyphenol; 4-[1′-phenyl-5-(trifluoromethyl)-1H,1′H-4,4′-bipyrazol-3-yl]benzene-1,3-diol; 4-[4-(1,3-benzothiazol-2-yl)-5-methyl-1H-pyrazol-3-yl]benzene-1,3-diol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]-1-methyl-1H-pyrazol-5-amine; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(1E)-3-(2-furyl)-3-oxoprop-1-en-1-yl]amino}benzoic acid; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-{[(2S)-2-ethylpiperidin-1-yl]methyl}-3-hydroxy-1-methyl-6H-benzo[c]chromen-6-one; 4-bromo-2-[(E)-(4H-1,2,4-triazol-4-ylimino)methyl]phenol; 4-bromo-2-[5-(2-furyl)-1H-pyrazol-3-yl]phenol; 4-bromo-6-chloro-2-oxo-1,3-benzoxathiol-5-yl ethyl carbonate; 4-ethyl-6-[4-(1-methyl-1H-benzimidazol-2-yl)-1H-pyrazol-3-yl]benzene-1,3-diol; 4-fluoro-N-[3-(trifluoromethyl)phenyl]benzamide; 4-hydroxy-3-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-2H-chromen-2-one; 4-hydroxy-3-propylquinolin-2(1H)-one; 4-hydroxy-5-phenyl-6H-pyrido[3,2,1-jk]carbazol-6-one; 4-hydroxy-8-methyl-3-{(E)-[(3R)-5-oxo-1,3-diphenylpyrazolidin-4-ylidene]methyl}quinolin -2(1H)-one; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-bromo-2-hydroxybenzoyl)-1-(2-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5-(benzoylamino)-N,N′-bis(2-hydroxyphenyl)isophthalamide; 5-(diethylamino)-2-{(E)-[(2-phenylethyl)imino]methyl}phenol; 5,7-dihydroxy-4-propyl-2H-chromen-2-one; 5-[(4-methylphenyl)thio]quinazoline-2,4-diamine; 5-{2-[(3,4-dichlorophenyl)thio]ethyl}-2-methylpyridine; 5-benzyl-3-phenyl-5H-pyrazolo[4,3-c]quinolines; 5-benzyl-4-hydroxy-6H-pyrido[3,2,1-jk]carbazol-6-one; 5-chloro-2-hydroxy-N-phenylbenzamide; 5-hydroxy-4-methyl-7-propyl-2H-chromen-2-one; 5-methoxy-2-[3-methyl-4-(1,3-thiazol-4-yl)isoxazol-5-yl]phenol; 5-methyl-2-[5-(2-thienyl)-1H-pyrazol-3-yl]phenol; 6-(4-chlorophenyl)-7-hydroxy-1,3-dimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione″6,6′-biquinoline; 6-[(S)-[4-(dimethylamino)phenyl](piperidin-1-yl)methyl]-1,3-benzodioxol-5-ol; 6-{[(2-ethylphenyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-{[(4-chlorophenyl)thio]methyl}-2-phenyl-1H-pyrazolo[3,4-b]pyridine-3,4(2H,7H)-dione; 6-{[(4-ethoxyphenyl)(methyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-allyl-7-hydroxy-4,8-dimethyl-2H-chromen-2-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-benzyl-7-hydroxy-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one; 6-bromo-2-(trifluoromethyl)quinolin-4-ol; 6-butyl-2-(2-furyl)-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidin-7-one; 6-chloro-2-(4-chlorophenyl)-1H-benzimidazol-1-ol; 6-chloro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-chloro-3-(4-methylphenyl)-3,4-dihydro-2H-1,3-benzoxazine; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 6-ethyl-7-hydroxy-3-(1-methyl-1H-benzimidazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 6-fluoro-4-hydroxy-3-phenylquinolin-2(1H)-one; 6-methoxy-N-[(1S)-1-methylpropyl]furo[2,3-b]quinoline-2-carboxamide; 6-phenyl[1,2,3,4]tetraazolo[1,5-b]pyridazin-7-ol; 7-(4-bromophenyl)-5-hydroxy-1,3-benzoxathiol-2-one; 7,8-dihydroxy-2-phenyl-4H-chromen-4-one; 7,8-dihydroxy-4-phenyl-2H-chromen-2-one; 7-[(2E)-2-(4-fluoro-3-phenoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[2-chloro-5-(trifluoromethyl)phenyl]-5-hydroxy-1,3-benzoxathiol-2-one; 7-{(2E)-2-[(2-fluorobiphenyl-4-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-benzyl-8-hydroxy-10,10-dimethyl-6,10-dihydropyrido[1,2-a]indol-6-one; 7-chloro-4-piperidinoquinoline; 7-chloro-N-(3-fluoro-4-methylphenyl)quinolin-4-amine; 7-chloro-N-[2-(dimethylamino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 7-hydroxy-5-methyl-3-(1-phenyl-1H-pyrazol-4-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 7-hydroxy-6-methyl-3-(4-methyl-1,3-thiazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 8-(trifluoromethoxy)-2-(trifluoromethyl)quinolin-4-ol; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-[(2E)-2-(5-bromo-2-methoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-{(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-methoxy-N,N-dimethyl-5H-pyrimido[5,4-b]indol-4-amine; allyl(3R,3′R,4′S,6′R,8′S,8a′S)-6′-{4-[2-({[(3S,6R,7S,8aS)-3-[4-(dimethylamino)butyl]-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-7-yl]carbonyl}oxy)ethoxy]phenyl}-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2,1-c][1,4]oxazine]-8′-carboxylate″bis[4-(dimethylamino)phenyl]methanone oxime; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COC(═O)[C@]1(Cc2ccc(O)c(CC═C(C)C)c2)OC(═O)C(═C1c3ccc(O)cc3)O; COc1cc(/C═C/2\Oc3cc(O)ccc3C2=O)ccc1O; COc1cc(ccc1O)c2oc3cc(O)cc(O)c3c(═O)c2O; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl(2E)-3-(2-hydroxy-5-nitrophenyl)acrylate; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; ethyl 4-(benzylamino)-6-ethoxyquinoline-3-carboxylate; ethyl 4-[({[(5R)-5-ethyl-4,6-dioxo-1,4,5,6-tetrahydropyrimidin-2-yl]thio}acetyl)amino]benzoate; ethyl 4-[(2-phenylethyl)amino]quinoline-3-carboxylate; ethyl 4-{[(2-anilino-2-oxoethyl)thio]methyl}-5-hydroxy-2-phenyl-1-benzofuran-3-carboxylate; ethyl 4-{[(2E)-3-(2-thienyl)prop-2-enoyl]amino}benzoate; ethyl 6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-{[(4-methylphenyl)thio]methyl}-1H-indole-3-carboxylate; ethyl 6-ethoxy-4-{[(1R)-1-methylpropyl]amino}quinoline-3-carboxylate; ethyl 6-methyl-4-[(4-morpholin-4-ylphenyl)amino]quinoline-3-carboxylate; isopropyl(2S)-2-{[(2S)-2-{[(2S,3R)-2-{[(2S)-2-amino-3-mercaptopropyl]amino}-3-methylpentyl ]oxy}-3-phenylpropanoyl]amino}-4-(methylsulfonyl)butanoate; methyl(2Z)-2-(4-hydroxybenzylidene)-3-oxo-2,3-dihydro-1-benzofuran-5-carboxylate; methyl 1-hydroxy-3-methylpyrido[1,2-a]benzimidazole-4-carboxylate; methyl 2,3-bis-O-(biphenyl-2-ylcarbamoyl)-4-O-[(3-ethylphenyl)carbamoyl]-alpha-L-idopyranoside; methyl 5-hydroxy-1-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylate; N-(1,3-benzodioxol-5-yl)-7-chloroquinolin-4-amine; N-(2,3-dihydro-1-benzofuran-5-ylcarbonyl)-2-hydroxybenzamide; N-(2,5-dimethylphenyl)benzamide; N-(2-chlorobenzyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(2-chlorobenzyl)-2-phenyl-1H-benzimidazole-5-sulfonamide; N-(2-ethoxyphenyl)-2-hydroxybenzamide; N-(2-hydroxy-4-methylphenyl)-4-[(methylthio)methyl]benzamide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(2-hydroxybenzoyl)-4-(trifluoromethyl)benzamide; N-(2-hydroxyphenyl)-8-[(2E)-2-(1-naphthylmethylene)hydrazino]-8-oxooctanamide; N-(3-bromo-4-hydroxy-1-naphthyl)-4-chlorobenzenesulfonamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-chlorophenyl)-4-(5-hydroxy-1-phenyl-1H-pyrazol-3-yl)piperidine-1-carbothioamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(3-hydroxypyridin-2-yl)-4-phenoxybenzamide; N-(3-imidazo[1,2-a]pyrimidin-2-ylphenyl)cyclopentanecarboxamide; N-(4-bromophenyl)-2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]acetamide; N-(4-carbamoylphenyl)-1-phenyl-3-(2-thienyl)-1H-pyrazole-4-carboxamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(4-fluorophenyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(5-{[(1S)-1-methylpropyl]thio}-1,3,4-thiadiazol-2-yl)-2-(trifluoromethyl)benzamide; N-(5-hydroxy-1-naphthyl)-4-methylbenzenesulfonamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-(6-methyl-1,3-benzothiazol-2(3H)-ylidene)thiophene-2-carboxamide; N-(cyclohexylcarbonyl)-2-hydroxybenzamide; N,2-diphenylquinazolin-4-amine; N,N,8-trimethyl-5H-pyrimido[5,4-b]indol-4-amine; N,N′-1H-isoindole-1,3(2H)-diylidenedianiline; N,N-diethyl-8-methyl-5H-pyrimido[5,4-b]indol-4-amine; N,N-dimethyl-4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzenesulfonamide; N-[(1E)-(9-ethyl-9H-carbazol-3-yl)methylene]-4H-1,2,4-triazol-4-amine; N-[(1E)-1H-indol-3-ylmethylene]-1-propyl-1H-benzimidazol-2-amine; N-[(1S)-1-benzylpropyl]-6-[(4-methylpiperidin-1-yl)sulfonyl]-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(3-chloro-1-benzothiophen-2-yl)carbonyl]-2-hydroxybenzamide; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N-[2-(1H-benzimidazol-2-yl)phenyl]-2-methylpropanamide; N-[2-chloro-5-(trifluoromethyl)phenyl]-2-(4,4-dimethyl-2,6-dioxocyclohexyl)acetamide; N-[2-hydroxy-3-(4-oxo-4H-chromen-2-yl)phenyl]acetamide; N-[3-(1,3-benzothiazol-2-yl)-4-hydroxyphenyl]-2,2-dimethylpropanamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]benzenesulfonamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]thiophene-2-sulfonamide; N-[4-(1H-benzimidazol-2-yl)phenyl]-2-(2-methoxyphenyl)acetamide; N-[4-(ethylsulfonyl)-2-hydroxyphenyl]benzamide; N-[5-(ethylsulfonyl)-2-hydroxyphenyl]-2-(4-methoxyphenoxy)acetamide; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diamine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; N-benzyl-2-hydroxybenzamide; N-benzyl-6-{[(3-methoxyphenyl)amino]sulfonyl}-N-methyl-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)/C═C/c4ccccc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3cCc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](Oc2c([C@H]3[C@@H](Oc4cc(O)cc(O)c4C3=O)c5ccc(O)cc5)c(O)cc(O)c2C1=O)c6ccc(O)cc6; O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O)c(O)c4) O[C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1=O)c26)[C@@H]3OC(═O)c7cc(O)c(O)c(O)c7; OC[C@H]1O[C@@H](OC [C@H]2O[C@@H](Oc3c(oc4cc(O)cc(O)c4c3=O)c5cCc(O)cc5)[C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O; and OC1[C@H](OC(═O)c2cc(O)c(O)c(O)c2)OC3COC(═O)c4cc(O)c(O)c(O)c4-c5c(O)c(O)c(O)cc5C(═O)O[C@@H]1[C@@H]3OC(═O)c6cc(O)c(O)c(O)c6c7c(O)c(O)c(O)cc7C(═O)OOc1ccc(cc1)[C@H]2CC(═O)c3c(O)cc(O)c([C@H]4[C@@H](Oc5cc(O)cc(O)c5C4=O)c6ccc(O)cc6) c3O2Oc1ccc2C(═O)/C(═C/c3ccc(O)c(O)c3)/Oc2c1.
26 . The method of claim 21 , wherein said method is used to treat or prevent malaria.
27 . A method of treating an individual infected with Plasmodium or Theileria or who has been or will be exposed to Plasmodium or Theileria , comprising the step of
providing said individual with one or more compounds that inhibit the ability of HDP to produce hemozoin from heme.
28 . The method of claim 27 , wherein said one or more compounds bind to heme.
29 . The method of claim 28 , wherein said one or more compounds prevent heme from binding to HDP.
30 . The method of claim 28 , wherein said one or more compounds allow the binding of heme to HDP but prevent detoxification of heme by HDP.
31 . The method of claim 27 , wherein said one or more compounds bind to HDP.
32 . The method of claim 31 , wherein said one or more compounds prevent binding of heme to HDP.
33 . The method of claim 31 , wherein said one or more compounds prevent the production of hemozoin from bound heme.
34 . The method of claim 31 , wherein said one or more compound bind at the active site of HDP.
35 . The method of claim 31 , wherein said one or more compound bind at an allosteric site of HDP.
36 . The method of claim 27 wherein said one or more compounds is selected from the group consisting of:
(1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)-3-(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1H-perimidine-2-carboxylic acid; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl}-1H-isoindole-1,3(2H)-dione; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-[(4-{[(2R)-tetrahydrofiuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl}oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimethylaniline; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chromen-4-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-chloro-N-[2-(dimethylamino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; N-(2-ethoxyphenyl)-2-hydroxybenzamide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diamine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; and O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O(O)O)c4) O[C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1=O)c26)[C@@H]3OC (═O)c7cc(O)c(O)c(O)c7.
37 . The method of claim 27 wherein said one or more compounds is selected from the group consisting of
(10S)-10-(dimethylamino)-9-methyl-7H,10H-naphtho[1,8-gh]chromen-7-one; (1E,4E)-1-[4-(dimethylamino)phenyl]-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one; (1R,3R)-1-isopropyl-2,3,4,9-tetrahydro-1H-beta-carboline-3-carboxylic acid; (1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E)-3-(3,4-dimethoxyphenyl)-N-(3,4-dimethylphenyl)acrylamide; (2E)-6-ethoxy-2-(2-hydroxybenzylidene)-1-benzothiophen-3(2H)-one; (2E)-N-(2-methyl-1,3-benzothiazol-6-yl)-3-phenylacrylamide; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2E,5Z)-2-[(2-chlorophenyl)imino]-5-(4-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (2R)-1-(benzylamino)-3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol; (2R)-2-(2,4-dichlorophenoxy)-N-(5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)propanamide; (2R)-2-[(5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid; (2R)-2-[(E)-2-(1,3-benzodioxol-5-yl)vinyl]-5,6-dimethyl-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-one; (2R,3Z)-6-chloro-3-[(dimethylamino)methylene]-2-methyl-2,3-dihydro-4H-thiochromen-4-one; (2S)-2-(4-chlorophenyl)-3-oxo-4-phenylbutanenitrile; (2S)-2-[(5E)-5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]succinic acid; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (2S,3Z)-3-(1H-indol-3-ylmethylene)-2-phenyl-2,3-dihydro-4H-chromen-4-one; (2Z)-2-acetamido-N-(3,5-dimethylphenyl)-3-phenylacrylamide; (2Z,5E)-2-[(3,5-dimethylphenyl)imino]-5-(2-hydroxy-3-methoxybenzylidene)-1,3-thiazolidin-4-one; (2Z,5Z)-2-[(2-chlorophenyl)imino]-5-(2-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (3,5-dichloro-2-hydroxyphenyl)(isoxazol-4-yl)methanone; (3-{(E)-[1-(3-fluorophenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl}-1H-indol-1-yl) acetonitrile; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3aS,6aS)-3-benzoyl-1,5-diphenyl-3a,6a-dihydropyrrolo[3,4-c]pyrazole-4,6(1H,5H)-dione; (3R)-3-(2-hydroxy-4-methylphenyl)-N-(2-methoxyphenyl)-3-phenylpropanamide; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; (3R,3′R,4′S,6′R,8′S,8a′S)-5-(4-hydroxybut-1-yn-1-yl)-6′-[4-(2-hydroxyethoxy)phenyl]-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2, 1-c][1,4]oxazine]-8′-carboxylic acid; (3S)-3-(2-hydroxy-4-methylbenzoyl)-2-(4-methylphenyl)isoindolin-1-one; (3S,3aR,6aR)-3-(5-bromo-2-hydroxyphenyl)-5-butyl-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazole-4,6(3H,5H)-dione; (3S,6S,7R,8aR)-3-(4-acetamidobutyl)-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazine-7-carboxylic acid; (3Z)-3-(3-hydroxy-4-methoxybenzylidene)-1-methyl-1,3-dihydro-2H-indol-2-one; (4E)-2-(4-methoxyphenyl)-4-[(4-methoxyphenyl)imino]-4H-chromen-6-ol; (4R)-3-(3,4-dichlorophenyl)-4-hydroxy-N-isopropyl-2-oxo-1,2,3,4-tetrahydroquinazoline-4-carboxamide; (4R)-4-(4-bromophenyl)-3-hydroxy-1-isopropyl-4,8-dihydro-1H-pyrazolo[3,4-e][1,4]thiazepin-7(6H)-one; (4R)-4-(4-ethylphenyl)-3-hydroxy-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4R)-5-(2-furylmethyl)-3-(2-hydroxyphenyl)-4-phenyl-4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H) -one; (4R)-N˜4˜-(6-chloro-2-methoxyacridin-9-yl)-N˜1˜,N˜1˜-diethylpentane-1,4-diamine; (4S)-4-(2-bromobenzoyl)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one; (4S)-4-(2-furyl)-3-hydroxy-7,7-dimethyl-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4S)-5,7-dihydroxy-4-phenylchroman-2-one; (4S,5S)-3,5-diphenyl-4,5-dihydro-1H-pyrazol-4-ol; (4S,7R)-2-amino-4-isobutyl-5-oxo-7-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile; (4Z)-2-[2-(4-chlorophenoxy)pyridin-3-yl]-4-[(dimethylamino)methylene]-1,3-oxazol-5(4H)-one; (5E)-1-(4-methylpentyl)-5-(1H-pyrrol-2-ylmethylene)pyrimidine-2,4,6(1H,3H,5H)-trione; (5E)-3-allyl-5-(2-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one; (5E)-5-[4-(diethylamino)benzylidene]-3-{[(2-methoxyphenyl)amino]methyl}-1,3-thiazolidine-2,4-dione; (5R)-5-methyl-4-phenyl-1,3,4-thiadiazolidine-2-thione; (5S,7R)-2,2-dimethyl-5,7-bis(2-phenylethyl)-7,8-dihydro-4H,5H-pyrano[4,3-d][1,3]dioxine; (5Z)-5-(4-hydroxybenzylidene)-3-[(2R)-tetrahydrofuran-2-ylmethyl]-2-thioxo-1,3-thiazolidin-4-one; (6E)-5-imino-6-{[1-(2-naphthyl)-1H-pyrrol-2-yl]methylene}-5,6-dihydro-7H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one; *c1ccccc1C2C(═O)N(C)c3ccccc3C2=O; [(2R)-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]acetic acid; [(5E)-4-oxo-5-(3-thienylmethylene)-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [(5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; {4-[(4-methylphenyl)sulfonyl]phenyl}hydrazine; 1-(2,4-dihydroxy-6-methylphenyl)-2-phenoxyethanone; 1-(2,4-dihydroxyphenyl)-2-(4-isopropylphenoxy)ethanone; 1-(3,4-dihydroxyphenyl)-2-({4-[(3,5-dimethoxyphenyl)amino]quinazolin-2-yl}thio)ethanone; 1-(4-chlorophenyl)-1-hydroxy-3-phenylurea; 1-(4-hydroxy-3,5-dimethylphenyl)-2-[(4-methylphenyl)thio]ethanone; 1-(4-iodo-2-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-ol; 1-(5-butyl-2,4-dihydroxyphenyl)-2-pyridin-2-ylethanone; 1-(5-ethyl-2,4-dihydroxyphenyl)-2-(1-methyl-1H-benzimidazol-2-yl)ethanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)-3-(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-[4-(7-chloroquinolin-4-yl)piperazino]propan-1-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1-ethynyl-2-phenoxybenzene; 1H-perimidine-2-carboxylic acid; 2-(1,3-benzodioxol-5-yl)-1-(2,4-dihydroxy-5-propylphenyl)ethanone; 2-(1H-benzimidazol-1-yl)-1-(5-ethyl-2,4-dihydroxyphenyl)ethanone; 2-(2,4-dichlorophenyl)-1H-imidazo[4,5-b]pyridin-1-ol; 2-(2,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,5-dihydroxy-7-methoxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-chlorophenyl)-4H-1,3-benzoxazin-4-one; 2-(4-chlorophenyl)-5-{[(4-pyridin-3-ylpyrimidin-2-yl)thio]methyl-2,4-dihydro-}H-pyrazol-3-one; 2-(4-fluoro-3-phenoxyphenyl)-3-hydroxy-4H-chromen-4-one; 2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)-N-(4-methylphenyl)acetamide; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(4-methylphenyl)-4H-1,3-benzoxazin-4-one; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2,2′-thiobis(4-chlorophenol); 2,4-dichloro-1-naphthyl[2,2,2-trifluoro-1-methyl-1-(trifluoromethyl)ethyl]carbamate; 2-[(2-phenoxyethyl)thio]quinazoline-4-thiol; 2-[(2R)-6,7-dimethyl-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]-N-ethylacetamide; 2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]-N-1-naphthylacetamide; 2-[(5S)-1-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-5-yl]phenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]phenol; 2-[5-(ethylsulfonyl)-2-hydroxyphenyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione; 2-{(1R)-1-[(1-allyl-1H-benzimidazol-2-yl)amino]ethyl}-4-chlorophenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl}-1H-isoindole-1,3(2H)-dione; 2-{[5-chloro-6-methyl-2-(2-pyridinyl)-4-pyrimidinyl]sulfanyl}-1-phenyl-1-ethanone; 2-amino-1-(2,4-dimethylphenyl)-1H-pyrrolo[2,3-b]quinoxaline-3-carbonitrile; 2-amino-5-butyl-4-(4-hydroxy-3-methoxyphenyl)-6-phenylnicotinonitrile; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-anilino-2-oxoethyl 2-(4-chlorobenzoyl)benzoate; 2-chloro-5-phenyl-3-pyridin-4-yl-4H-1,4-thiazine; 2-chloro-8-hydroxy-10,10-dimethyl-7-phenylpyrido[1,2-a]indol-6(10H)-one; 2-hydrazino-4,6-diphenylpyrimidine; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-methylphenyl)benzamide; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 2-hydroxy-N-[(4-methyl-2-phenyl-1,3-thiazol-5-yl)carbonyl]benzamide; 2-hydroxy-N-[2-(2-methoxyphenyl)acetyl]benzamide; 2-hydroxy-N-{[2-(4-methylphenoxy)-3-pyridinyl]carbonyl}benzamide; 2-hydroxy-N-pyridin-3-ylbenzamide; 2-phenyl-4H-thiochromene-4-thione; 2-phenyl-5-({[5-(trifluoromethyl)pyridin-2-yl]sulfonyl}methyl)-2,4-dihydro-3H-pyrazol-3-one; 2-phenyl-5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3-one; 3-(1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)-N-(2-hydroxyphenyl)-N-(4-methoxybenzyl)propanamide; 3-(1-acetyl-1H-indol-3-yl)-4-hydroxy-2H-chromen-2-one; 3-(1H-benzimidazol-1-yl)-6-ethyl-7-hydroxy-4H-chromen-4-one; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(3-{[(4-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(4-bromophenyl)-7-hydroxy-2-methyl-4H-chromen-4-one; 3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)propan-1-one; 3-(5-{(Z)-[5-(4-methylphenyl)-2-oxofuran-3(2H)-ylidene]methyl}-2-furyl)benzoic acid; 3-(quinazolin-4-ylamino)phenyl thiophene-2-carboxylate; 3,4-dimethoxy-N-(4-methyl-1,3-benzothiazol-2-yl)benzamide; 3,5-dichloro-2-hydroxybenzaldehyde N-tert-butyl-N′-methylthiosemicarbazone; 3-[(4-{[(2R)-tetrahydrofuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[2-(4-methoxyphenyl)ethyl]-10-methyl-6-phenyl-3,4-dihydro-2H,8H-chromeno[6,7-e][1,3]oxazin-8-one; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 3-{2-[(1,3-dioxo-1,3-dihydro-2H-inden-2-ylidene)methyl]-1H-pyrrol-1-yl}benzoic acid; 3-benzyl-4-hydroxy-1,2-dihydroquinolin-2-one; 3-benzyl-4-hydroxy-1-phenylquinolin-2(1H)-one; 3-benzyl-5,6-bis(4-methoxyphenyl)furo[2,3-d]pyrimidin-4(3H)-imine; 3-benzyl-5-ethyl-4-hydroxy-6-phenyl-1-(1,3-thiazol-2-yl)pyridin-2(1H)-one; 3-benzyl-6-ethoxy-4-hydroxyquinolin-2(1H)-one; 3-chloro-N-[2-(methylthio)-1,3-benzothiazol-6-yl]benzamide; 3-hydroxy-N-(2-methylphenyl)-2-naphthamide; 3-methoxy-2-methyl-6-[1′-phenyl-5-(trifluoromethyl)-1H,1′H-4,4′-bipyrazol-3-yl]phenol; 3-methoxy-N-(3-[1,3]oxazolo[4,5-b]pyridin-2-ylphenyl)benzamide; 3-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-5-ol; 3-methyl-1-phenyl-4-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[3,4-b]pyridin-6-one; 3-methyl-4-[(4-methylphenyl)thio]-1-phenyl-1H-pyrazol-5-yl methoxyacetate; 3-oxo-3-[3-({[3-(trifluoromethyl)phenyl]thio}methyl)phenyl]propanenitrile; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl}oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimnethylaniline; 4-(1-propyl-1H-benzimidazol-2-yl)aniline; 4-(2,6-dichlorobenzyl)-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-[(2,3,5,6-tetrafluoro-1,4-phenylene)bis(oxy)]diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(3S,6S,7R,8aR)-7-{[2-(4-{(3S,3′S,4′R,6′R,8′R,8a′R)-8′-[(allyloxy)carbonyl]-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2,1-c][1,4]oxazin]-6′-yl}phenoxy)ethoxy]carbonyl}-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-3-yl]-N,N,N-trimethylbutan-1-aminium; 4-[(4-chlorophenyl)thio]-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[1-(4-hydroxy-3-methoxybenzyl)-1H-benzimidazol-2-yl]-2-methoxyphenol; 4-[1′-phenyl-5-(trifluoromethyl)-1H,1′H-4,4′-bipyrazol-3-yl]benzene-1,3-diol; 4-[4-(1,3-benzothiazol-2-yl)-5-methyl-1H-pyrazol-3-yl]benzene-1,3-diol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]-1-methyl-1H-pyrazol-5-amine; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(1E)-3-(2-furyl)-3-oxoprop-1-en-1-yl]amino}benzoic acid; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-{[(2S)-2-ethylpiperidin-1-yl]methyl}-3-hydroxy-1-methyl-6H-benzo[c]chromen-6-one; 4-bromo-2-[(E)-(4H-1,2,4-triazol-4-ylimino)methyl]phenol; 4-bromo-2-[5-(2-furyl)-1H-pyrazol-3-yl]phenol; 4-bromo-6-chloro-2-oxo-1,3-benzoxathiol-5-yl ethyl carbonate; 4-ethyl-6-[4-(1-methyl-1H-benzimidazol-2-yl)-1H-pyrazol-3-yl]benzene-1,3-diol; 4-fluoro-N-[3-(trifluoromethyl)phenyl]benzamide; 4-hydroxy-3-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-2H-chromen-2-one; 4-hydroxy-3-propylquinolin-2(1H)-one; 4-hydroxy-5-phenyl-6H-pyrido[3,2,1-jk]carbazol-6-one; 4-hydroxy-8-methyl-3-{(E)-[(3R)-5-oxo-1,3-diphenylpyrazolidin-4-ylidene]methyl}quinolin -2(1H)-one; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-bromo-2-hydroxybenzoyl)-1-(2-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5-(benzoylamino)-N,N′-bis(2-hydroxyphenyl)isophthalamide; 5-(diethylamino)-2-{(E)-[(2-phenylethyl)imino]methyl}phenol; 5,7-dihydroxy-4-propyl-2H-chromen-2-one; 5-[(4-methylphenyl)thio]quinazoline-2,4-diamine; 5-{2-[(3,4-dichlorophenyl)thio]ethyl}-2-methylpyridine; 5-benzyl-3-phenyl-5H-pyrazolo[4,3-c]quinolines; 5-benzyl-4-hydroxy-6H-pyrido[3,2,1-jk]carbazol-6-one; 5-chloro-2-hydroxy-N-phenylbenzamide; 5-hydroxy-4-methyl-7-propyl-2H-chromen-2-one; 5-methoxy-2-[3-methyl-4-(1,3-thiazol-4-yl)isoxazol-5-yl]phenol; 5-methyl-2-[5-(2-thienyl)-1H-pyrazol-3-yl]phenol; 6-(4-chlorophenyl)-7-hydroxy-1,3-dimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione″6,6′-biquinoline; 6-[(S)-[4-(dimethylamino)phenyl](piperidin-1-yl)methyl]-1,3-benzodioxol-5-ol; 6-{[(2-ethylphenyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-{[(4-chlorophenyl)thio]methyl}-2-phenyl-1H-pyrazolo[3,4-b]pyridine-3,4(2H,7H)-dione; 6-{[(4-ethoxyphenyl)(methyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-allyl-7-hydroxy-4,8-dimethyl-2H-chromen-2-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-benzyl-7-hydroxy-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one; 6-bromo-2-(trifluoromethyl)quinolin-4-ol; 6-butyl-2-(2-furyl)-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidin-7-one; 6-chloro-2-(4-chlorophenyl)-1H-benzimidazol-1-ol; 6-chloro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-chloro-3-(4-methylphenyl)-3,4-dihydro-2H-1,3-benzoxazine; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 6-ethyl-7-hydroxy-3-(1-methyl-1H-benzimidazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 6-fluoro-4-hydroxy-3-phenylquinolin-2(1H)-one; 6-methoxy-N-[(1S)-1-methylpropyl]furo[2,3-b]quinoline-2-carboxamide; 6-phenyl[1,2,3,4]tetraazolo[1,5-b]pyridazin-7-ol; 7-(4-bromophenyl)-5-hydroxy-1,3-benzoxathiol-2-one; 7,8-dihydroxy-2-phenyl-4H-chromen-4-one; 7,8-dihydroxy-4-phenyl-2H-chromen-2-one; 7-[(2E)-2-(4-fluoro-3-phenoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[2-chloro-5-(trifluoromethyl)phenyl]-5-hydroxy-1,3-benzoxathiol-2-one; 7-{(2E)-2-[(2-fluorobiphenyl-4-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-benzyl-8-hydroxy-10,10-dimethyl-6,10-dihydropyrido[1,2-a]indol-6-one; 7-chloro-4-piperidinoquinoline; 7-chloro-N-(3-fluoro-4-methylphenyl)quinolin-4-amine; 7-chloro-N-[2-(dimethylamino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 7-hydroxy-5-methyl-3-(1-phenyl-1H-pyrazol-4-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 7-hydroxy-6-methyl-3-(4-methyl-1,3-thiazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 8-(trifluoromethoxy)-2-(trifluoromethyl)quinolin-4-ol; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-[(2E)-2-(5-bromo-2-methoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-{(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-methoxy-N,N-dimethyl-5H-pyrimido[5,4-b]indol-4-amine; allyl(3R,3′R,4′S,6′R,8′S,8a′S)-6′-{4-[2-({[(3S,6R,7S,8aS)-3-[4-(dimethylamino)butyl]-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-7-yl]carbonyl}oxy)ethoxy]phenyl}-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2,1-c][1,4]oxazine]-8′-carboxylate″bis[4-(dimethylamino)phenyl]methanone oxime; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COC(═O)[C@]1(Cc2ccc(O)c(CC═C(C)C)c2)OC(═O)C(═C1c3ccc(O)cc3)O; COc1cc(/C═C/2\Oc3cc(O)ccc3C2=O)ccc1O; COc1cc(ccc1O)c2oc3cc(O)cc(O)c3c(═O)c2O; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl(2E)-3-(2-hydroxy-5-nitrophenyl)acrylate; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; ethyl 4-(benzylamino)-6-ethoxyquinoline-3-carboxylate; ethyl 4-[({[(5R)-5-ethyl-4,6-dioxo-1,4,5,6-tetrahydropyrimidin-2-yl]thio}acetyl)amino]benzoate; ethyl 4-[(2-phenylethyl)amino]quinoline-3-carboxylate; ethyl 4-{[(2-anilino-2-oxoethyl)thio]methyl}-5-hydroxy-2-phenyl-1-benzofuran-3-carboxylate; ethyl 4-{[(2E)-3-(2-thienyl)prop-2-enoyl]amino}benzoate; ethyl 6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-{[(4-methylphenyl)thio]methyl}-1H-indole-3-carboxylate; ethyl 6-ethoxy-4-{[(1R)-1-methylpropyl]amino}quinoline-3-carboxylate; ethyl 6-methyl-4-[(4-morpholin-4-ylphenyl)amino]quinoline-3-carboxylate; isopropyl (2S)-2-{[(2S)-2-{[(2S,3R)-2-{[(2S)-2-amino-3-mercaptopropyl]amino}-3-methylpentyl]oxy}-3-phenylpropanoyl]amino}-4-(methylsulfonyl)butanoate; methyl(2Z)-2-(4-hydroxybenzylidene)-3-oxo-2,3-dihydro-1-benzofuran-5-carboxylate; methyl 1-hydroxy-3-methylpyrido[1,2-a]benzimidazole-4-carboxylate; methyl 2,3-bis-O-(biphenyl-2-ylcarbamoyl)-4-O-[(3-ethylphenyl)carbamoyl]-alpha-L-idopyranoside; methyl 5-hydroxy-1-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylate; N-(1,3-benzodioxol-5-yl)-7-chloroquinolin-4-amine; N-(2,3-dihydro-1-benzofuran-5-ylcarbonyl)-2-hydroxybenzamide; N-(2,5-dimethylphenyl)benzamide; N-(2-chlorobenzyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(2-chlorobenzyl)-2-phenyl-1H-benzimidazole-5-sulfonamide; N-(2-ethoxyphenyl)-2-hydroxybenzamide; N-(2-hydroxy-4-methylphenyl)-4-[(methylthio)methyl]benzamide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(2-hydroxybenzoyl)-4-(trifluoromethyl)benzamide; N-(2-hydroxyphenyl)-8-[(2E)-2-(1-naphthylmethylene)hydrazino]-8-oxooctanamide; N-(3-bromo-4-hydroxy-1-naphthyl)-4-chlorobenzenesulfonamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-chlorophenyl)-4-(5-hydroxy-1-phenyl-1H-pyrazol-3-yl)piperidine-1-carbothioamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(3-hydroxypyridin-2-yl)-4-phenoxybenzamide; N-(3-imidazo[1,2-a]pyrimidin-2-ylphenyl)cyclopentanecarboxamide; N-(4-bromophenyl)-2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]acetamide; N-(4-carbamoylphenyl)-1-phenyl-3-(2-thienyl)-1H-pyrazole-4-carboxamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(4-fluorophenyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(5-{[(1S)-1-methylpropyl]thio}-1,3,4-thiadiazol-2-yl)-2-(trifluoromethyl)benzamide; N-(5-hydroxy-1-naphthyl)-4-methylbenzenesulfonamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-(6-methyl-1,3-benzothiazol-2(3H)-ylidene)thiophene-2-carboxamide; N-(cyclohexylcarbonyl)-2-hydroxybenzamide; N,2-diphenylquinazolin-4-amine; N,N,8-trimethyl-5H-pyrimido[5,4-b]indol-4-amine; N,N′-1H-isoindole-1,3(2H)-diylidenedianiline; N,N-diethyl-8-methyl-5H-pyrimido[5,4-b]indol-4-amine; N,N-dimethyl-4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzenesulfonamide; N-[(1E)-(9-ethyl-9H-carbazol-3-yl)methylene]-4H-1,2,4-triazol-4-amine; N-[(1E)-1H-indol-3-ylmethylene]-1-propyl-1H-benzimidazol-2-amine; N-[(1S)-1-benzylpropyl]-6-[(4-methylpiperidin-1-yl)sulfonyl]-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(3-chloro-1-benzothiophen-2-yl)carbonyl]-2-hydroxybenzamide; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N-[2-(1H-benzimidazol-2-yl)phenyl]-2-methylpropanamide; N-[2-chloro-5-(trifluoromethyl)phenyl]-2-(4,4-dimethyl-2,6-dioxocyclohexyl)acetamide; N-[2-hydroxy-3-(4-oxo-4H-chromen-2-yl)phenyl]acetamide; N-[3-(1,3-benzothiazol-2-yl)-4-hydroxyphenyl]-2,2-dimethylpropanamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]benzenesulfonamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]thiophene-2-sulfonamide; N-[4-(1H-benzimidazol-2-yl)phenyl]-2-(2-methoxyphenyl)acetamide; N-[4-(ethylsulfonyl)-2-hydroxyphenyl]benzamide; N-[5-(ethylsulfonyl)-2-hydroxyphenyl]-2-(4-methoxyphenoxy)acetamide; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diamine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; N-benzyl-2-hydroxybenzamide; N-benzyl-6-{[(3-methoxyphenyl)amino]sulfonyl}-N-methyl-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)/C═C/c4ccccc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](Oc2c([C@H]3[C@@H](Oc4cc(O)cc(O)c4C3=O)c5ccc(O)cc5)c(O)cc(O)c2C1=O)c6ccc(O)cc6; O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O)c(O)c4)O[C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1=O)c26)[C@@H]3OC(═O)c7cc(O)c(O)c(O)c7; OC[C@H]1O[C@@H](OC[C@H]2O[C@@H](Oc3c(oc4cc(O)cc(O)c4c3=O)c5ccc(O)cc5)[C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O; and OC1[C@H](OC(═O)c2cc(O)c(O)c(O)c2)OC3COC(═O)c4cc(O)c(O)c(O)c4-c5c(O)c(O)c(O)cc5C(═O)O[C@@H]1[C @@H]3OC(═O)c6cc(O)c(O)c(O)c6c7c(O)c(O)c(O)cc7C(═O)OOc1ccc(cc1)[C@H]2CC(═O)c3c(O)cc(O)c([C@H]4[C@@H](Oc5cc(O)cc(O)c5C4=O)c6ccc(O)cc6) c3020c1ccc2C(═O)/C(═C/c3ccc(O)c(O)c3)/Oc2c1.
38 . A method for identifying compounds that inhibit HDP expression, comprising the steps of
a) contacting Plasmodium with a test compound and b) determining whether said Plasmodium expresses HDP.
39 . The method of claim 38 , wherein said step of determining is carried out by measuring mRNA.
40 . The method of claim 38 , wherein said step of determining is carried out by measuring HDP.
41 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and an antimalarially effective amount of at least one compound selected from the group consisting of:
(1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)-3-(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1H-perimidine-2-carboxylic acid; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl-1H-isoindole-1,3(2H)-dione; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-[(4-{[(2R)-tetrahydrofuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimethylaniline; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chromen-4-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-chloro-N-[2-(dimethylarnino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; N-(2-ethoxyphenyl)-2-hydroxybenzarnide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diarnine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(o)c(O)c2)O[C@@H](Oc3ccc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; and O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O)c(O)c4) O[C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1=O)c26)[C(@H]3OC(═O)c7cc(O)c(O)c(O)c7.
42 . A pharmaceutical composition comprising a pharmnaceutically acceptable carrier and an antimalarially effective amount of at least one compound selected from the group consisting of
(10S)-10-(dimethylamino)-9-methyl-7H,10H-naphtho[1,8-gh]chromen-7-one; (1E,4E)-1-[4-(dimethylamino)phenyl]-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one; (1R,3R)-1-isopropyl-2,3,4,9-tetrahydro-1H-beta-carboline-3-carboxylic acid; (1S)-1-(3,4-dichlorophenyl)-2-(2-imino-1,3-benzothiazol-3(2H)-yl)ethanol; (2E)-2-[(pyridin-3-ylamino)methylene]-1-benzothiophen-3(2H)-one; (2E)-3-(3,4-dimethoxyphenyl)-N-(3,4-dimethylphenyl)acrylamide; (2E)-6-ethoxy-2-(2-hydroxybenzylidene)-1-benzothiophen-3(2H)-one; (2E)-N-(2-methyl-1,3-benzothiazol-6-yl)-3-phenylacrylamide; (2E,5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-2-(phenylimino)-1,3-thiazolidin-4-one; (2E,5Z)-2-[(2-chlorophenyl)imino]-5-(4-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (2R)-1-(benzylamino)-3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol; (2R)-2-(2,4-dichlorophenoxy)-N-(5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)propanamide; (2R)-2-[(5Z)-5-(4-hydroxy-3,5-dimethoxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid; (2R)-2-[(E)-2-(1,3-benzodioxol-5-yl)vinyl]-5,6-dimethyl-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-one; (2R,3Z)-6-chloro-3-[(dimethylarnino)methylene]-2-methyl-2,3-dihydro-4H-thiochromen-4-one; (2S)-2-(4-chlorophenyl)-3-oxo-4-phenylbutanenitrile; (2S)-2-[(5E)-5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]succinic acid; (2S)-N-(4-chlorophenyl)-2-methyl-2,3-dihydro-4H-1,4-benzoxazine-4-carboxamide; (2S,3Z)-3-(1H-indol-3-ylmethylene)-2-phenyl-2,3-dihydro-4H-chromen-4-one; (2Z)-2-acetamido-N-(3,5-dimethylphenyl)-3-phenylacrylamide; (2Z,5E)-2-[(3,5-dimethylphenyl)imino]-5-(2-hydroxy-3-methoxybenzylidene)-1,3-thiazolidin-4-one; (2Z,5Z)-2-[(2-chlorophenyl)imino]-5-(2-hydroxy-3-nitrobenzylidene)-1,3-thiazolidin-4-one; (3,5-dichloro-2-hydroxyphenyl)(isoxazol-4-yl)methanone; (3-{(E)-[1-(3-fluorophenyl)-2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene]methyl}-1H-indol-1-yl) acetonitrile; (3aR,4R,9bR)-8-chloro-4-(4-chlorophenyl)-9-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-6-ol; (3aS,6aS)-3-benzoyl-1,5-diphenyl-3a,6a-dihydropyrrolo[3,4-c]pyrazole-4,6(1H,5H)-dione; (3R)-3-(2-hydroxy-4-methylphenyl)-N-(2-methoxyphenyl)-3-phenylpropanamide; (3R)-5,7-dichloro-3-hydroxy-3-(2-methylimidazo[1,2-a]pyridin-3-yl)-1,3-dihydro-2H-indol-2-one; (3R,3′R,4′S,6′R,8′S,8a′S)-5-(4-hydroxybut-1-yn-1-yl)-6′-[4-(2-hydroxyethoxy)phenyl]-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2, 1-c][1,4]oxazine]-8′-carboxylic acid; (3S)-3-(2-hydroxy-4-methylbenzoyl)-2-(4-methylphenyl)isoindolin-1-one; (3S,3aR,6aR)-3-(5-bromo-2-hydroxyphenyl)-5-butyl-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazole-4,6(3H,5H)-dione; (3S,6S,7R,8aR)-3-(4-acetamidobutyl)-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazine-7-carboxylic acid; (3Z)-3-(3-hydroxy-4-methoxybenzylidene)-1-methyl-1,3-dihydro-2H-indol-2-one; (4E)-2-(4-methoxyphenyl)-4-[(4-methoxyphenyl)imino]-4H-chromen-6-ol; (4R)-3-(3,4-dichlorophenyl)-4-hydroxy-N-isopropyl-2-oxo-1,2,3,4-tetrahydroquinazoline-4-carboxamide; (4R)-4-(4-bromophenyl)-3-hydroxy-1-isopropyl-4,8-dihydro-1H-pyrazolo[3,4-e][1,4]thiazepin-7(6H)-one; (4R)-4-(4-ethylphenyl)-3-hydroxy-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4R)-5-(2-furylmethyl)-3-(2-hydroxyphenyl)-4-phenyl-4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H) -one; (4R)-N˜4˜-(6-chloro-2-methoxyacridin-9-yl)-N˜1˜,N˜1˜-diethylpentane-1,4-diamine; (4S)-4-(2-bromobenzoyl)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one; (4S)-4-(2-furyl)-3-hydroxy-7,7-dimethyl-2-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one; (4S)-5,7-dihydroxy-4-phenylchroman-2-one; (4S,5S)-3,5-diphenyl-4,5-dihydro-1H-pyrazol-4-ol; (4S,7R)-2-amino-4-isobutyl-5-oxo-7-phenyl-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile; (4Z)-2-[2-(4-chlorophenoxy)pyridin-3-yl]-4-[(dimethylamino)methylene]-1,3-oxazol-5(4H)-one; (5E)-1-(4-methylpentyl)-5-(1H-pyrrol-2-ylmethylene)pyrimidine-2,4,6(1H,3H,5H)-trione; (5E)-3-allyl-5-(2-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one; (5E)-5-[4-(diethylamino)benzylidene]-3-{[(2-methoxyphenyl)amino]methyl}-1,3-thiazolidine-2,4-dione; (5R)-5-methyl-4-phenyl-1,3,4-thiadiazolidine-2-thione; (5S,7R)-2,2-dimethyl-5,7-bis(2-phenylethyl)-7,8-dihydro-4H,5H-pyrano[4,3-d][1,3]dioxine; (5Z)-5-(4-hydroxybenzylidene)-3-[(2R)-tetrahydrofuran-2-ylmethyl]-2-thioxo-1,3-thiazolidin-4-one; (6E)-5-imino-6-{[1-(2-naphthyl)-1H-pyrrol-2-yl]methylene}-5,6-dihydro-7H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one; *c1ccccc1C2C(═O)N(C)c3ccccc3C2=O; [(2R)-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]acetic acid; [(5E)-4-oxo-5-(3-thienylmethylene)-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [(5E)-5-(5-bromo-3-chloro-2-hydroxybenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone; {4-[(4-methylphenyl)sulfonyl]phenyl}hydrazine; 1-(2,4-dihydroxy-6-methylphenyl)-2-phenoxyethanone; 1-(2,4-dihydroxyphenyl)-2-(4-isopropylphenoxy)ethanone; 1-(3,4-dihydroxyphenyl)-2-({4-[(3,5-dimethoxyphenyl)amino]quinazolin-2-yl}thio)ethanone; 1-(4-chlorophenyl)-1-hydroxy-3-phenylurea; 1-(4-hydroxy-3,5-dimethylphenyl)-2-[(4-methylphenyl)thio]ethanone; 1-(4-iodo-2-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-ol; 1-(5-butyl-2,4-dihydroxyphenyl)-2-pyridin-2-ylethanone; 1-(5-ethyl-2,4-dihydroxyphenyl)-2-(1-methyl-1H-benzimidazol-2-yl)ethanone; 1,2,3,4,6-pentakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose; 1-[(2S)-3-(9H-carbazol-9-yl)-2-hydroxypropyl]-8-hydroxyquinolinium; 1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one; 1-[4-(7-chloroquinolin-4-yl)piperazino]propan-1-one; 1-ethyl-6-methoxy-4-methyl-2-[(Z)-(3-methyl-1,3-thiazol-2(3H)-ylidene)methyl]benzo[h]quinolinium; 1-ethynyl-2-phenoxybenzene; 1H-perimidine-2-carboxylic acid; 2-(1,3-benzodioxol-5-yl)-1-(2,4-dihydroxy-5-propylphenyl)ethanone; 2-(1H-benzimidazol-1-yl)-1-(5-ethyl-2,4-dihydroxyphenyl)ethanone; 2-(2,4-dichlorophenyl)-1H-imidazo[4,5-b]pyridin-1-ol; 2-(2,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,5-dihydroxy-7-methoxy-4H-chromen-4-one; 2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-4H-chromen-4-one; 2-(4-chlorophenyl)-4H-1,3-benzoxazin-4-one; 2-(4-chlorophenyl)-5-{[(4-pyridin-3-ylpyrimidin-2-yl)thio]methyl}-2,4-dihydro-3H-pyrazol-3-one; 2-(4-fluoro-3-phenoxyphenyl)-3-hydroxy-4H-chromen-4-one; 2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)-N-(4-methylphenyl)acetamide; 2-(4-methoxyphenyl)-4H-1,3-benzoxazin-4-one; 2-(4-methoxyphenyl)pyridin-3-ol; 2-(4-methylphenyl)-4H-1,3-benzoxazin-4-one; 2-(morpholin-4-ylmethyl)-1-naphthol; 2,2′-buta-1,3-diyne-1,4-diyldiphenol; 2,2′-thiobis(4-chlorophenol); 2,4-dichloro-1-naphthyl[2,2,2-trifluoro-1-methyl-1-(trifluoromethyl)ethyl]carbamate; 2-[(2-phenoxyethyl)thio]quinazoline-4-thiol; 2-[(2R)-6,7-dimethyl-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]-N-ethylacetamide; 2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]-N-1-naphthylacetamide; 2-[(5S)-1-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-5-yl]phenol; 2-[(E)-(6-methoxy-1-methylquinolin-2(1H)-ylidene)methyl]-3-methyl-1,3-benzothiazol-3-ium; 2-[(Z)-(3-ethyl-6-methoxy-1,3-benzothiazol-2(3H)-ylidene)methyl]-1,6-dimethylquinolinium; 2-[2-(4-hydroxyphenyl)ethyl]-6-methylpyridin-3-ol; 2-[4-(1-benzofuiran-2-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]-5-methoxyphenol; 2-[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]phenol; 2-[5-(ethylsulfonyl)-2-hydroxyphenyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione; 2-{(1R)-1-[(1-allyl-1H-benzimidazol-2-yl)amino]ethyl}-4-chlorophenol; 2-{(3R)-1-[4-(2-hydroxyethoxy)benzyl]piperidin-3-yl}-1H-isoindole-1,3(2H)-dione; 2-{[5-chloro-6-methyl-2-(2-pyridinyl)-4-pyrimidinyl]sulfanyl}-1-phenyl-1-ethanone; 2-amino-1-(2,4-dimethylphenyl)-1H-pyrrolo[2,3-b]quinoxaline-3-carbonitrile; 2-amino-5-butyl-4-(4-hydroxy-3-methoxyphenyl)-6-phenylnicotinonitrile; 2-amino-8-(azepan-1-ylmethyl)-3-(1,3-benzothiazol-2-yl)-7-hydroxy-4H-chromen-4-one; 2-anilino-2-oxoethyl 2-(4-chlorobenzoyl)benzoate; 2-chloro-5-phenyl-3-pyridin-4-yl-4H-1,4-thiazine; 2-chloro-8-hydroxy-10,10-dimethyl-7-phenylpyrido[1,2-a]indol-6(10H)-one; 2-hydrazino-4,6-diphenylpyrimidine; 2-hydrazino-4-methylquinoline; 2-hydroxy-N-(4-methylphenyl)benzamide; 2-hydroxy-N-(4-propylbenzoyl)benzamide; 2-hydroxy-N-[(4-methyl-2-phenyl-1,3-thiazol-5-yl)carbonyl]benzamide; 2-hydroxy-N-[2-(2-methoxyphenyl)acetyl]benzamide; 2-hydroxy-N-{[2-(4-methylphenoxy)-3-pyridinyl]carbonyl}benzamide; 2-hydroxy-N-pyridin-3-ylbenzamide; 2-phenyl-4H-thiochromene-4-thione; 2-phenyl-5-({[5-(trifluoromethyl)pyridin-2-yl]sulfonyl}methyl)-2,4-dihydro-3H-pyrazol-3-one; 2-phenyl-5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3-one; 3-(1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)-N-(2-hydroxyphenyl)-N-(4-methoxybenzyl)propanamide; 3-(1-acetyl-1H-indol-3-yl)-4-hydroxy-2H-chromen-2-one; 3-(1H-benzimidazol-1-yl)-6-ethyl-7-hydroxy-4H-chromen-4-one; 3-(2-hydroxy-5-methoxybenzoyl)-2-(4-methylphenyl)isoindolin-1-one; 3-(3-{[(2-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(3-{[(4-chlorophenyl)thio]methyl}phenyl)-3-oxopropanenitrile; 3-(4-bromophenyl)-7-hydroxy-2-methyl-4H-chromen-4-one; 3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)propan-1-one; 3-(5-{(Z)-[5-(4-methylphenyl)-2-oxofuran-3(2H)-ylidene]methyl}-2-furyl)benzoic acid; 3-(quinazolin-4-ylamino)phenyl thiophene-2-carboxylate; 3,4-dimethoxy-N-(4-methyl-1,3-benzothiazol-2-yl)benzamide; 3,5-dichloro-2-hydroxybenzaldehyde N-tert-butyl-N′-methylthiosemicarbazone; 3-[(4-{[(2R)-tetrahydrofuran-2-ylmethyl]amino}quinazolin-2-yl)amino]phenol; 3-[2-(4-methoxyphenyl)ethyl]-10-methyl-6-phenyl-3,4-dihydro-2H,8H-chromeno[6,7-e][1,3]oxazin-8-one; 3-[4-(9H-fluoren-9-yl)piperazin-1-yl]-N-[3-(trifluoromethyl)phenyl]propanamide; 3-{2-[(1,3-dioxo-1,3-dihydro-2H-inden-2-ylidene)methyl]-1H-pyrrol-1-yl}benzoic acid; 3-benzyl-4-hydroxy-1,2-dihydroquinolin-2-one; 3-benzyl-4-hydroxy-1-phenylquinolin-2(1H)-one; 3-benzyl-5,6-bis(4-methoxyphenyl)furo[2,3-d]pyrimidin-4(3H)-imine; 3-benzyl-5-ethyl-4-hydroxy-6-phenyl-1-(1,3-thiazol-2-yl)pyridin-2(1H)-one; 3-benzyl-6-ethoxy-4-hydroxyquinolin-2(1H)-one; 3-chloro-N-[2-(methylthio)-1,3-benzothiazol-6-yl]benzamide; 3-hydroxy-N-(2-methylphenyl)-2-naphthamide; 3-methoxy-2-methyl-6-[1′-phenyl-5-(trifluoromethyl)-1H,1′H-4,4′-bipyrazol-3-yl]phenol; 3-methoxy-N-(3-[1,3]oxazolo[4,5-b]pyridin-2-ylphenyl)benzamide; 3-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-5-ol; 3-methyl-1-phenyl-4-(trifluoromethyl)-1,7-dihydro-6H-pyrazolo[3,4-b]pyridin-6-one; 3-methyl-4-[(4-methylphenyl)thio]-1-phenyl-1H-pyrazol-5-yl methoxyacetate; 3-oxo-3-[3-({[3-(trifluoromethyl)phenyl]thio}methyl)phenyl]propanenitrile; 4-({(2S)-3-[4-(diphenylmethyl)piperazin-1-yl]-2-hydroxypropyl}oxy)-1H-indole-2-carbonitrile; 4-(1H-benzimidazol-2-yl)-N,N-dimethylaniline; 4-(1-propyl-1H-benzimidazol-2-yl)aniline; 4-(2,6-dichlorobenzyl)-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4-(7-methylimidazo[1,2-a]pyridin-2-yl)benzene-1,2-diol; 4,4′-(4-phenyl-1H-imidazole-2,5-diyl)diphenol; 4,4′-[(2,3,5,6-tetrafluoro-1,4-phenylene)bis(oxy)]diphenol; 4,4′-methylenebis(3-hydroxy-2-naphthoic acid)-3,3′-[(4-iminocyclohexa-2,5-dien-1-ylidene)methylene]dianiline (1:1); 4,4′-propane-2,2-diylbis(2-chlorophenol); 4-[(3S,6S,7R,8aR)-7-{[2-(4-{(3S,3′S,4′R,6′R,8′R,8a′R)-8′-[(allyloxy)carbonyl]-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2,1-c][1,4]oxazin]-6′-yl}phenoxy)ethoxy]carbonyl}-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-3-yl]-N,N,N-trimethylbutan-1-aminium; 4-[(4-chlorophenyl)thio]-3-methyl-1-phenyl-1H-pyrazol-5-ol; 4-[(5S)-5-(4-fluorophenyl)-1-(4-nitrophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenol; 4-[1-(4-hydroxy-3-methoxybenzyl)-1H-benzimidazol-2-yl]-2-methoxyphenol; 4-[1′-phenyl-5-(trifluoromethyl)-1H,1′H-4,4′-bipyrazol-3-yl]benzene-1,3-diol; 4-[4-(1,3-benzothiazol-2-yl)-5-methyl-1H-pyrazol-3-yl]benzene-1,3-diol; 4-[4-(3,4-dihydro-2H-1,5-benzodioxepin-7-yl)-3-methylisoxazol-5-yl]benzene-1,3-diol; 4-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]-1-methyl-1H-pyrazol-5-amine; 4-[5-[5-(4-methylpiperazin-1-yl)-3H-benzoimidazol-2-yl]-1,3-dihydrobenzoimidazol-2-ylidene]cyclohexa-2,5-dien-1-one; 4-{[(1E)-3-(2-furyl)-3-oxoprop-1-en-1-yl]amino}benzoic acid; 4-{[(2-ethylphenyl)amino]methyl}-5-(hydroxymethyl)-2-methylpyridin-3-ol; 4-{[(2S)-2-ethylpiperidin-1-yl]methyl}-3-hydroxy-1-methyl-6H-benzo[c]chromen-6-one; 4-bromo-2-[(E)-(4H-1,2,4-triazol-4-ylimino)methyl]phenol; 4-bromo-2-[5-(2-furyl)-1H-pyrazol-3-yl]phenol; 4-bromo-6-chloro-2-oxo-1,3-benzoxathiol-5-yl ethyl carbonate; 4-ethyl-6-[4-(1-methyl-H 1H-benzimidazol-2-yl)-H 1H-pyrazol-3-yl]benzene-1,3-diol; 4-fluoro-N-[3-(trifluoromethyl)phenyl]benzamide; 4-hydroxy-3-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]-2H-chromen-2-one; 4-hydroxy-3-propylquinolin-2(11)-one; 4-hydroxy-5-phenyl-6H-pyrido[3,2,1-jk]carbazol-6-one; 4-hydroxy-8-methyl-3-{(E)-[(3R)-5-oxo-1,3-diphenylpyrazolidin-4-ylidene]methyl}quinolin-2(1H)-one; 4-phenylquinolin-2-amine; 5-(2-hydroxy-5-methylbenzoyl)-1-(4-methylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-bromo-2-hydroxybenzoyl)-1-(2-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile; 5-(5-chloro-2-hydroxybenzoyl)-2-oxo-N,1-diphenyl-1,2-dihydropyridine-3-carboxamide; 5-(benzoylamino)-N,N′-bis(2-hydroxyphenyl)isophthalamide; 5-(diethylamino)-2-{(E)-[(2-phenylethyl)imino]methyl}phenol; 5,7-dihydroxy-4-propyl-2H-chromen-2-one; 5-[(4-methylphenyl)thio]quinazoline-2,4-diamine; 5-{2-[(3,4-dichlorophenyl)thio]ethyl}-2-methylpyridine; 5-benzyl-3-phenyl-5H-pyrazolo[4,3-c]quinolines; 5-benzyl-4-hydroxy-6H-pyrido[3,2,1-jk]carbazol-6-one; 5-chloro-2-hydroxy-N-phenylbenzamide; 5-hydroxy-4-methyl-7-propyl-2H-chromen-2-one; 5-methoxy-2-[3-methyl-4-(1,3-thiazol-4-yl)isoxazol-5-yl]phenol; 5-methyl-2-[5-(2-thienyl)-1H-pyrazol-3-yl]phenol; 6-(4-chlorophenyl)-7-hydroxy-1,3-dimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione″6,6′-biquinoline; 6-[(S)-[4-(dimethylamino)phenyl](piperidin-1-yl)methyl]-1,3-benzodioxol-5-ol; 6-{[(2-ethylphenyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-{[(4-chlorophenyl)thio]methyl}-2-phenyl-1H-pyrazolo[3,4-b]pyridine-3,4(2H,7H)-dione; 6-{[(4-ethoxyphenyl)(methyl)amino]sulfonyl}-4-oxo-N-[(2S)-tetrahydrofuran-2-ylmethyl]-1,4-dihydroquinoline-3-carboxamide; 6-allyl-7-hydroxy-4, 8-dimethyl-2H-chromen-2-one; 6-amino-1-ethylbenzo[cd]indol-2(1H)-one; 6-benzyl-7-hydroxy-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one; 6-bromo-2-(trifluoromethyl)quinolin-4-ol; 6-butyl-2-(2-furyl)-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidin-7-one; 6-chloro-2-(4-chlorophenyl)-1H-benzimidazol-1-ol; 6-chloro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-chloro-3-(4-methylphenyl)-3,4-dihydro-2H-1,3-benzoxazine; 6-chloro-3-[2-(4-chlorophenyl)ethyl]-3,4-dihydro-2H-1,3-benzoxazine; 6-ethyl-7-hydroxy-3-(1-methyl-1H-benzimidazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 6-fluoro-4-hydroxy-3-phenylquinolin-2(1H)-one; 6-methoxy-N-[(1S)-1-methylpropyl]furo[2,3-b]quinoline-2-carboxamide; 6-phenyl[1,2,3,4]tetraazolo[1,5-b]pyridazin-7-ol; 7-(4-bromophenyl)-5-hydroxy-1,3-benzoxathiol-2-one; 7,8-dihydroxy-2-phenyl-4H-chromen-4-one; 7,8-dihydroxy-4-phenyl-2H-chromen-2-one; 7-[(2E)-2-(4-fluoro-3-phenoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[(2E)-2-(biphenyl-4-ylmethylene)hydrazino]-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-[2-chloro-5-(trifluoromethyl)phenyl]-5-hydroxy-1,3-benzoxathiol-2-one; 7-{(2E)-2-[(2-fluorobiphenyl-4-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-7-oxoheptanamide; 7-benzyl-8-hydroxy-10,10-dimethyl-6,10-dihydropyrido[1,2-a]indol-6-one; 7-chloro-4-piperidinoquinoline; 7-chloro-N-(3-fluoro-4-methylphenyl)quinolin-4-amine; 7-chloro-N-[2-(dimethylamino)ethyl]-4H-thieno[3,2-c]thiochromene-2-carboxamide; 7-chloro-N-phenylquinolin-4-amine; 7-hydroxy-2-methyl-6-propyl-3-pyridin-2-yl-4H-chromen-4-one; 7-hydroxy-5-methy1-3-(1-phenyl-1H-pyrazol-4-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 7-hydroxy-6-methyl-3-(4-methyl-1,3-thiazol-2-yl)-2-(trifluoromethyl)-4H-chromen-4-one; 8-(trifluoromethoxy)-2-(trifluoromethyl)quinolin-4-ol; 8-[(2E)-2-(2-bromobenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-[(2E)-2-(5-bromo-2-methoxybenzylidene)hydrazino]-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-{(2E)-2-[(6-bromo-1,3-benzodioxol-5-yl)methylene]hydrazino}-N-(2-hydroxyphenyl)-8-oxooctanamide; 8-methoxy-N,N-dimethyl-5H-pyrimido[5,4-b]indol-4-amine; allyl(3R,3′R,4′S,6′R,8′S,8a′S)-6′-{4-[2-({[(3S,6R,7S,8aS)-3-[4-(dimethylamino)butyl]-6-(4-hydroxyphenyl)-1,4-dioxooctahydropyrrolo[1,2-a]pyrazin-7-yl]carbonyl}oxy)ethoxy]phenyl}-5-iodo-1′,2-dioxo-3′,4′-diphenyl-1,2,3′,4′,8′,8a′-hexahydro-1′H-spiro[indole-3,7′-pyrrolo[2,1-c][1,4]oxazine]-8′-carboxylate″bis[4-(dimethylamino)phenyl]methanone oxime; CN(C)c1ccc2N=c3cc(C)c(N)cc3=Sc2c1; COC(═O)[C@]1(Cc2ccc(O)c(CC═C(C)C)c2)OC(═O)C(═C1c3ccc(O)cc3)O; COc1cc(/C═C/2\Oc3cc(O)ccc3C2=O)ccc1O; COc1cc(ccc1O)c2oc3cc(O)cc(O)c3c(═O)c2O; COc1cc(O)c-2c(CCc3cc(OC)c(OC)cc32)c1; ethyl(2E)-3-(2-hydroxy-5-nitrophenyl)acrylate; ethyl 1-benzyl-4-[(dimethylamino)methyl]-5-hydroxy-2-phenyl-1H-indole-3-carboxylate; ethyl 2-ethoxy-5-hydroxy-1H-benzo[g]indole-3-carboxylate; ethyl 4-(benzylamino)-6-ethoxyquinoline-3-carboxylate; ethyl 4-[({[(5R)-5-ethyl-4,6-dioxo-1,4,5,6-tetrahydropyrimidin-2-yl]thio}acetyl)amino]benzoate; ethyl 4-[(2-phenylethyl)amino]quinoline-3-carboxylate; ethyl 4-}[(2-anilino-2-oxoethyl)thio]methyl}-5-hydroxy-2-phenyl-1-benzofuran-3-carboxylate; ethyl 4-{[(2E)-3-(2-thienyl)prop-2-enoyl]amino}benzoate; ethyl 6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-{[(4-methylphenyl)thio]methyl}-1H-indole-3-carboxylate; ethyl 6-ethoxy-4-{[(1R)-1-methylpropyl]amino}quinoline-3-carboxylate; ethyl 6-methyl-4-[(4-morpholin-4-ylphenyl)amino]quinoline-3-carboxylate; isopropyl(2S)-2-{[(2S)-2-{[(2S,3R)-2-{[(2S)-2-amino-3-mercaptopropyl]amino}-3-methylpentyl]oxy}-3-phenylpropanoyl]amino}-4-(methylsulfonyl)butanoate; methyl(2Z)-2-(4-hydroxybenzylidene)-3-oxo-2,3-dihydro-1-benzofuran-5-carboxylate; methyl 1-hydroxy-3-methylpyrido[1,2-a]benzimidazole-4-carboxylate; methyl 2,3-bis-O-(biphenyl-2-ylcarbamoyl)-4-O-[(3-ethylphenyl)carbamoyl]-alpha-L-idopyranoside; methyl 5-hydroxy-1-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxylate; N-(1,3-benzodioxol-5-yl)-7-chloroquinolin-4-amine; N-(2,3-dihydro-1-benzofuran-5-ylcarbonyl)-2-hydroxybenzamide; N-(2,5-dimethylphenyl)benzamide; N-(2-chlorobenzyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(2-chlorobenzyl)-2-phenyl-1H-benzimidazole-5-sulfonamide; N-(2-ethoxyphenyl)-2-hydroxybenzamide; N-(2-hydroxy-4-methylphenyl)-4-[(methylthio)methyl]benzamide; N-(2-hydroxybenzoyl)-2-thiophenecarboxamide; N-(2-hydroxybenzoyl)-3-methoxybenzamide; N-(2-hydroxybenzoyl)-4-(trifluoromethyl)benzamide; N-(2-hydroxyphenyl)-8-[(2E)-2-(1-naphthylmethylene)hydrazino]-8-oxooctanamide; N-(3-bromo-4-hydroxy-1-naphthyl)-4-chlorobenzenesulfonamide; N-(3-chloro-4-hydroxy-1-naphthyl)-4-ethoxybenzenesulfonamide; N-(3-chlorophenyl)-4-(5-hydroxy-1-phenyl-1H-pyrazol-3-yl)piperidine-1-carbothioamide; N-(3-furylcarbonyl)-2-hydroxybenzamide; N-(3-hydroxypyridin-2-yl)-4-phenoxybenzamide; N-(3-imidazo[1,2-a]pyrimidin-2-ylphenyl)cyclopentanecarboxamide; N-(4-bromophenyl)-2-[(3-cyano-4-methyl-6-oxo-1,6-dihydropyridin-2-yl)thio]acetamide; N-(4-carbamoylphenyl)-1-phenyl-3-(2-thienyl)-1H-pyrazole-4-carboxamide; N-(4-ethylbenzoyl)-2-hydroxybenzamide; N-(4-fluorophenyl)-2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)acetamide; N-(5-{[(1S)-1-methylpropyl]thio}-1,3,4-thiadiazol-2-yl)-2-(trifluoromethyl)benzamide; N-(5-hydroxy-1-naphthyl)-4-methylbenzenesulfonamide; N-(6-chloro-2-phenyl-4H-chromen-4-ylidene)-1-(2-furyl)methanamine; N-(6-methyl-1,3-benzothiazol-2(3H)-ylidene)thiophene-2-carboxamide; N-(cyclohexylcarbonyl)-2-hydroxybenzamide; N,2-diphenylquinazolin-4-amine; N,N,8-trimethyl-5H-pyrimido[5,4-b]indol-4-amine; N,N′-1H-isoindole-1,3(2H)-diylidenedianiline; N,N-diethyl-8-methyl-5H-pyrimido[5,4-b]indol-4-amine; N,N-dimethyl-4-(6-methylimidazo[1,2-a]pyridin-2-yl)benzenesulfonamide; N-[(1E)-(9-ethyl-9H-carbazol-3-yl)methylene]-4H-1,2,4-triazol-4-amine; N-[(1E)-1H-indol-3-ylmethylene]-1-propyl-1H-benzimidazol-2-amine; N-[(1S)-1-benzylpropyl]-6-[(4-methylpiperidin-1-yl)sulfonyl]-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-[(1S)-1-phenylethyl]quinazolin-4-amine; N-[(3-chloro-1-benzothiophen-2-yl)carbonyl]-2-hydroxybenzamide; N-[(4E)-2-(4-methoxyphenyl)-6-methyl-4H-chromen-4-ylidene]-2-phenylethanamine; N-[2-(1H-benzimidazol-2-yl)phenyl]-2-methylpropanamide; N-[2-chloro-5-(trifluoromethyl)phenyl]-2-(4,4-dimethyl-2,6-dioxocyclohexyl)acetamide; N-[2-hydroxy-3-(4-oxo-4H-chromen-2-yl)phenyl]acetamide; N-[3-(1,3-benzothiazol-2-yl)-4-hydroxyphenyl]-2,2-dimethylpropanamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]benzenesulfonamide; N-[3-(1,3-benzothiazol-2-ylthio)-4-hydroxyphenyl]thiophene-2-sulfonamide; N-[4-(1H-benzimidazol-2-yl)phenyl]-2-(2-methoxyphenyl)acetamide; N-[4-(ethylsulfonyl)-2-hydroxyphenyl]benzamide; N-[5-(ethylsulfonyl)-2-hydroxyphenyl]-2-(4-methoxyphenoxy)acetamide; N4-(3,5-dichlorophenyl)-6-methylpyrimidine-2,4-diamine; N-benzo[g]quinolin-4-yl-N′-isopropylbenzene-1,4-diamine; N-benzyl-2-hydroxybenzamide; N-benzyl-6-{[(3-methoxyphenyl)amino]sulfonyl}-N-methyl-4-oxo-1,4-dihydroquinoline-3-carboxamide; N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c)c(c(O)c2)O[C@@H](Oc3ccc(C(═O)/C═C/c4ccccc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](O)[C@@H](COC(═O)c2cc(O)c(O)c(O)c2)O[C@@H](Oc3ccc(C(═O)CCc4ccc(O)cc4)c(O)c3)[C@@H]1O; O[C@H]1[C@@H](Oc2c([C@H]3[C@@H](Oc4cc(O)cc(O)c4C3=O)c5ccc(O)cc5)c(O)cc(O)c2C=O)c6ccc(O)cc6; O[C@H]1[C@H]2[C@H](CC(═O)O)C(═O)O[C@@H]3C(COC(═O)c4cc(O)c(O)c(O)c4) O[C@@H](OC(═O)c5cc(O)c(O)c(O)c5)C(OC(═O)c6cc(O)c(O)c(OC1=O)c26)[C@@H]3OC (═O)c7cc(O)c(O)c(O)c7; OC[C@H]1O[C@@H](OC[C@H]2O[C@@H](Oc3c(oc4cc(O)cc(O)c4c3=O)c5ccc(O)cc5)[C@H](O)[C@@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O; and OC1[C@H](OC(═O)c2cc(O)c(O)c(O)c2)OC3COC(═O)c4cc(O)c(O)c(O)c4-cc(O)c(O)c(O)cc5C(═O)O[C@@H]1[C@@H]3OC(═O)c6cc(O)c(O)c(O)c6c7c(O)c(O)c(O)cc7C(═O)OOc1ccc(cc1)[C@H]2CC(═O)c3c(O)cc(O)c([C@H]4[C@@H](Oc5cc(O)cc(O)c5C4=O)c6ccc(O)cc6) c3O2Oc1ccc2C(═O)/C(═C/c3ccc(O)c(O)c3)/Oc2c1.Join the waitlist — get patent alerts
Track US2007148185A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.