Squaric acid: a valuable scaffold for developing antimalarials?

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

http://hdl.handle.net/10451/9635

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We describe here the synthesis of a library of thirty-eight squaric derivatives and the evaluation of activity against papain-, falcipain-2- and a chloroquine-resistant strain of P. falciparum. The most active compounds combine signiﬁcant antiplasmodial activity with minimal cytotoxicity.