In vitro antimalarial activity of novel trifluoromethyl- and bis(trifluoromethyl)quinoline derivatives

The In vitro antimalarial activity of a series of 2- and 8-trifluoromethyl- and 2,8-bis(trifluoromethyl) quinoline-4-(5-pyrimidino) and N4-ethyl-5-nit rolmidazolo)methylene ketones was assessed against the chloroquine-sensitiv e strain (D10) of Plasmodium falciparum. Although the in vitro antimalarial activity of these compounds is more or less of the same order of magnitude , derivatives containing two trifluoromethyl groups achieve a slightly high er in vitro activity than compounds with one trifluoromethyl group, with 2, 8-bis(trifluoromethyl) quinoline-4-(N4-ethyl-5-nitroimidazolo) methylene an d 2,8-bis(trifluoromethyl) quinoline-4-(5-pyrimidino) ketones showing IC50 of 4,8 and 5,2 mug/ml, respectively. These compounds seem to bind to DNA by intercalation.