Aza vinyl sulfones: Synthesis and evaluation as antiplasmodial agents

Glória, Paulo M. C.; Gut, Jiri; Gonçalves, Lídia M.; Rosenthal, Philip J.; Moreira, Rui; Santos, Maria M. M.

http://hdl.handle.net/10451/8155

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Abstract(s)

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 IC50 values between 0.95 and 4.5 μM, suggesting that these are potential lead compounds for the development of new antimalarial agents.