Synthesis and in vitro evaluation shows disquaramide compounds are a promising class of anti-leishmanial drugs

Abstract

ABSTRACTAn increasing number of treatment failures with current pharmaceutics, as well as a lack of a vaccine, demonstrates the need to develop new treatment options for leishmaniasis. Herein, we describe the synthesis and in vitro analysis of 24 disquaramide compounds targeting theLeishmania majorparasite. Of the compounds that were evaluated, six of them (13,19,20,22,24, and26) were capable of significantly decreasing the number of parasites by up to 42% compared to the control by day four. This demonstrates that disquaramides either impair parasite replication or have leishmancidal effects. Additionally, none of the disquaramide compounds tested displayed host cell cytotoxicity. These experiments provide evidence that disquaramides have the potential to be effective anti-leishmanial therapeutics.