Antiplasmodial activity of naphthoquinones related to lapachol and beta-lapachone

The in vitro antiplasmodial activity of 26 naphthoquinone derivatives related to the natural lapachol (1) and beta-lapachone (2) was tested. Ten of these derivatives are reported for the first time. The evaluation was performed on cultures of F32 strain of Plasmodium falciparum, and some derivatives displayed attractive ill vitro activities (IC50 < 10 mu M). Based on these results, some structure-activity relationships have been determined.