Squaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agents

Ribeiro, Carlos J. A.; Kumar, S. P.; Gut, Jiri; Gonçalves, Lidia M.; Rosenthal, Philip J.; Moreira, Rui; Santos, Maria M. M.

http://hdl.handle.net/10451/17885

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Autores

Ribeiro, Carlos J. A.

Resumo(s)

We report the synthesis and structure–activity relationship (SAR) analysis of a series of hybrid compounds containing a squaric moiety conjugated with heterocyclic moieties from well-known antimalarials. This novel series of compounds presents improved antiplasmodial activity compared with the squaric derivatives described in our previous work. Three compounds, 8b (IC50 = 99 nM), 8c (IC50 = 95 nM), and 8d (IC50 = 105 nM) had greater in vitro potency than chloroquine 1 (IC50 = 140 nM) against chloroquine resistant Plasmodium falciparum. In addition, they were noncytotoxic against NIH 3T3 and Hek 293T cells.