Aza vinyl sulfones: Synthesis and evaluation as antiplasmodial agents

作者:Gloria Paulo M C; Gut Jiri; Goncalves Lidia M; Rosenthal Philip J; Moreira Rui; Santos Maria M M*
来源:Bioorganic & Medicinal Chemistry, 2011, 19(24): 7635-7642.
DOI:10.1016/j.bmc.2011.10.018

摘要

A series of novel aza vinyl sulfones were designed, synthesized in good yields and evaluated as antiplasmodial agents. Tested compounds did not show activity against papain or the Plasmodium falciparum cysteine protease falcipain-2. However, a number of the new compounds effectively inhibited the in vitro development of P. falciparum. Compounds containing a squaramide group were the most active, with IC(50) values between 0.95 and 4.5 mu M, suggesting that these are potential lead compounds for the development of new antimalarial agents.