Novel anti-neurodegenerative natural compounds isolated from Alpiniae Oxyphyllae Fructus and their total synthesis

Abstract

This invention is directed to novel compounds isolated or derived from Alpiniae oxyphyllae fructus, chemically synthesized novel compounds, methods of preparing the novel compounds and uses thereof as neuroprotectants or drugs for treating neurodegenerative diseases such as Parkinson's disease.

1 . A compound with Formula I: 
       
         
           
           
               
               
           
         
         wherein R 1  and R 3  are independently selected from the group consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenly, alkynyl, aryl, heteroaryl, carboxy, alkyloxy, hydroxyl, amino, nitro, alkylthio, acyl, cyano, acylamino, halo and ester; and 
         R 2  and R 4  are independently selected from the group consisting of H, unsubstituted or substituted alkyl, cycloalkyl, aryl, heteroaryl, alkyoxy, acyl, acylamino and halo. 
       
     
     
         2 . The compound of  claim 1 , wherein R 1  and R 3  are independently unsubstituted or substituted (C1-C3) alkyl; and R 2  and R 4  are H. 
     
     
         3 . The compound of  claim 1 , wherein said compound is an isolated and purified ((R)-4-(2-hydroxy-5-methylphenyl)-5-methylhexanoic acid). 
     
     
         4 . The compound of  claim 1 , wherein said compound is hydroxy-5-methylphenyl)-5-methylhexanoic acid) or (4-(2-hydroxy-5-methylphenyl)-5-methylhexanoic acid). 
     
     
         5 .- 8 . (canceled) 
     
     
         9 . A method of treating Parkinson's disease, or protecting against neural damage or neural cells loss, comprising the step of administering said compound of  claim 1  to a subject in need. 
     
     
         10 . A method of treating neurodegenerative disease in a human patient comprising administrating to the patient a therapeutically effective amount of said compound of  claim 1  and chrysin, wherein said compound exhibits a synergistic effect with said chrysin for neuroprotective effect. 
     
     
         11 .- 31 . (canceled)