2. Academic Validation
  3. Synthesis and evaluation of original amidoximes as antileishmanial agents

Synthesis and evaluation of original amidoximes as antileishmanial agents

  • Bioorg Med Chem. 2010 Oct 15;18(20):7310-20. doi: 10.1016/j.bmc.2010.06.099.
Ahlem Bouhlel 1,  Christophe Curti,  Aurélien Dumètre,  Michèle Laget,  Maxime D Crozet,  Nadine Azas,  Patrice Vanelle
Affiliations

Affiliation

  • 1 Laboratoire de Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, Universités d'Aix-Marseille I, II, et III-CNRS, UMR 6264, 13385 Marseille cedex 05, France.
PMID: 20833057 DOI: 10.1016/j.bmc.2010.06.099
Abstract

An original series of amidoxime derivatives was synthesized using manganese(III) acetate, Buchwald-Hartwig and Heck reactions. Two amidoximes (39 and 52) showed interesting in vitro activities toward Leishmania donovani promastigotes, exhibiting 8.3 and 8.8 μM IC(50) values. Moreover, the cytotoxicity of these compounds was evaluated on human THP1 cells, giving access to the corresponding selectivity index. Among the 25 tested compounds, amidoximes 38 and 39 and diamidoximes 50 and 52 exhibited a better selectivity index than pentamidine used as a drug compound reference.

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