Design, synthesis and in vitro antimalarial activity of an acylhydrazone library

Patricia Melnyk (1) , Virginie A. Leroux (1) , Christian Sergheraert (1) , Philippe Grellier (2)

1 SSFB - Synthèse, structure et fonction des biomolécules
2 MCAM - Molécules de Communication et Adaptation des Micro-Organismes

A library of acylhydrazone iron chelators was synthesized and tested for its ability to inhibit the growth of a chloroquine-resistant strain of Plasmodium falciparum. Some of these new compounds are significantly more active than desferrioxamine DFO, the iron chelator in widespread clinical use and also than the most effective chelators.

Domaines: Chimie thérapeutique

Patricia Melnyk, Virginie A. Leroux, Christian Sergheraert, Philippe Grellier. Design, synthesis and in vitro antimalarial activity of an acylhydrazone library. Bioorganic and Medicinal Chemistry Letters, 2006, 16, pp.31-35. ⟨hal-00097328⟩