Covalent Inhibitors of <i>Plasmodium falciparum</i> Glyceraldehyde 3-Phosphate Dehydrogenase with Antimalarial Activity in Vitro

Abstract

Covalent inhibitors of <i>Pf</i>GAPDH characterized by a 3-bromoisoxazoline warhead were developed, and their mode of interaction with the target enzyme was interpreted by means of molecular modeling studies: some of them displayed a submicromolar antiplasmodial activity against both chloroquine sensitive and resistant strains of <i>Plasmodium falciparum</i>, with good selectivity indices.