Aryl-alkyl-lysines: small molecular membrane-active antiplasmodial agents

Abstract

Due to emerging resistance there is a steady need for new antimalarial drugs. Here, we report a new class of water soluble, non-toxic compounds, aryl-alkyl-lysines, with promising activity against the ring stage of Plasmodium falciparum. The optimal compound perturbed the plasma membrane potential and the digestive vacuole of parasites. In the murine model of malaria (Plasmodium berghei ANKA) the compound was able to increase the survival of mice by at least 5 days by an intra-peritoneal route. Further, the compounds showed no apparent toxicity to mice at the concentration tested.