Antimalarial benzo[c]phenanthridines

Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC50 below 5 ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC50 below 30 ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.

Graphical abstractAnalogues of the antimalarial alkaloid nitidine have been prepared with IC50 in vitro in the low nanomolar range against chloroquine-resistant Plasmodium falciparum.Figure optionsDownload full-size imageDownload as PowerPoint slide