Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):396-401. doi: 10.1016/j.bmcl.2007.10.027.
Pierre Verhaeghe  1 ,  Nadine Azas ,  Monique Gasquet ,  Sébastien Hutter ,  Christophe Ducros ,  Michèle Laget ,  Sylvain Rault ,  Pascal Rathelot ,  Patrice Vanelle
Affiliations
  • 1. Laboratoire de Chimie Organique Pharmaceutique, UMR CNRS 6517, Faculté de Pharmacie, Université de la Méditerranée, 27 Bd. Jean Moulin, 13385 Marseille Cedex 05, France.
PMID: 17981462 DOI: 10.1016/j.bmcl.2007.10.027
Abstract

A series of original 4-aryl-substituted 2-trichloromethylquinazoline derivatives was synthesized using a microwave-assisted Suzuki-Miyaura cross-coupling approach. Antiplasmodial activity was evaluated on both chloroquino-resistant and -sensitive Plasmodium falciparum strains, and the selectivity indexes for THP1 and HepG2 human cells were also calculated, revealing their antiplasmodial potential.