2. Academic Validation
  3. Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines

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

Affiliation

  • 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.

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