Ribeiro, Carlos J. A.Kumar, S. P.Gut, JiriGonçalves, Lidia M.Rosenthal, Philip J.Moreira, RuiSantos, Maria M. M.2015-04-132015-04-132013European Journal of Medicinal Chemistry 69 (2013) 365-372http://hdl.handle.net/10451/17885We 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.engSquaramide4-AminoquinolineMalariaHybridAntiplasmodial activityjournal articlehttp://dx.doi.org/10.1016/j.ejmech.2013.08.037