Design, synthesis, and biological activities of conformationally restricted analogs of primaquine with a 1,10-phenanthroline framework
作者:Cheikh Sall、Ange-Désiré Yapi、Nicolas Desbois、Séverine Chevalley、Jean-Michel Chezal、Kimny Tan、Jean-Claude Teulade、Alexis Valentin、Yves Blache
DOI:10.1016/j.bmcl.2008.07.013
日期:2008.8
A series of primaquine analogs was prepared, according to a conformationally restricted conformation of primaquine. In vitro antiplasmodial activities were evaluated and showed that all compounds were active on different strains of Plasmodium falciparum. In particular compounds 5 and 15 possessing a methoxy group were more active than was primaquine. Furthermore, analog 5 displayed good in vitro gametocytocidal
根据伯氨喹的构象受限构象,制备了一系列伯氨喹类似物。评价了体外抗血浆活性,并表明所有化合物对不同菌株的恶性疟原虫均具有活性。特别地,具有甲氧基的化合物5和15比伯氨喹更具活性。此外,类似物5表现出良好的体外杀细胞活性。此外,针对Vero细胞系的细胞毒性活性计算了选择性指数。