作者: Aurélie Leverrier , Joanne Bero , Julián Cabrera , Michel Frédérich , Joëlle Quetin-Leclercq
DOI: 10.1016/J.EJMECH.2015.05.044
关键词:
摘要: In this work, a series of hybrid compounds were tested as antiparasitic substances. These hybrids prepared from bile acids and Cinchona alkaloids by the formation covalent C-C bond via decarboxylative Barton-Zard reaction between two entities. The showed only weak properties, but all exhibited high in vitro activities (IC50: 0.48-5.39 μM) against Trypanosoma brucei. more active than their respective parent (up to 135 fold increase in activity), displayed good selectivity indices. Aditionally, these inhibited growth chloroquine-sensitive strain Plasmodium falciparum (3D7: IC50: 36.1 nM 8.72 μM), most had IC50s comparable that artemisinin 36 nM). Some structure-activity relationships among group 48 are discussed. activity may be explained an improvement bioavailability, since lipophilic derivatives lowest IC50s.