Chemical Strategies towards the Synthesis of Betulinic Acid and Its More Potent Antiprotozoal Analogues

摘要: Betulinic acid (BA, 3β-hydroxy-lup-20(29)-en-28-oic acid) is a pentacyclic triterpene present predominantly in Betula ssp. (Betulaceae) and also widely spread many species belonging to different plant families. BA presents wide spectrum of remarkable pharmacological properties, such as cytotoxic, anti-HIV, anti-inflammatory, antidiabetic antimicrobial activities, including antiprotozoal effects. The review first describes the sources discusses chemical strategies produce this molecule starting from betulin, its natural precursor. Next, properties are briefly discussed for synthesis analogues displaying antiplasmodial, antileishmanial antitrypanosomal activities systematically presented. antiplasmodial activity described was moderate, nevertheless, some C-3 position acylated showed an improvement hybrid models-with artesunic acid-showed most interesting properties. Some presented more intense compared with BA, and, addition these, heterocycles fused C-2/C-3 positions amide derivatives were promising analogues. Regarding activity, prepared by formation at C-28 carboxylic group lupane skeleton. Considering that can be produced either isolation extracts or transformation easily obtained ssp., it could said great interest material novel agents.