title: Synthesis and evaluation of original amidoximes as antileishmanial agents.
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.
authors.affiliation: Laboratoire de Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, Universités d'Aix-Marseille I, II, et III-CNRS, UMR 6264, 13385 Marseille cedex 05, France.
authors.forename: Ahlem
authors.initials: A
authors.lastname: Bouhlel
authors.forename: Christophe
authors.initials: C
authors.lastname: Curti
authors.forename: Aurélien
authors.initials: A
authors.lastname: Dumètre
authors.forename: Michèle
authors.initials: M
authors.lastname: Laget
authors.forename: Maxime D
authors.initials: MD
authors.lastname: Crozet
authors.forename: Nadine
authors.initials: N
authors.lastname: Azas
authors.forename: Patrice
authors.initials: P
authors.lastname: Vanelle
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002460:Cell Line; D003500:Cyclization; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects; D008345:Manganese / Q000737:chemistry; D010084:Oxidation-Reduction; D010091:Oximes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D010091:Oximes; D008345:Manganese