Preparation and Antimalarial Activities of “Trioxaquines”, New Modular Molecules with a Trioxane Skeleton Linked to a 4-Aminoquinoline

Abstract

Trioxaquines are new antimalarial drugs which combine two active fragments (an aminoquinoline and a trioxane) with independant modes of action covalently linked within a single molecule. This strategy, which can be characterized as a “covalent bitherapy”, allowed us to obtain modular molecules with high antimalarial activity in vitro either on chloroquine sensitive or on chloroquine resistant Plasmodium falciparum strains.