Synthesis and evaluation of original amidoximes as antileishmanial agents

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• 作者：Ahlem Bouhlel ; Christophe Curti ; Auré ; lien Dumè ; tre ; Michè ; le Laget ; Maxime D. Crozet ; Nadine Azas ; Patrice Vanelle
• 关键词：Amidoximes ; Antileishmanial ; Dihydrofuran
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：15 October 2010
• 年：2010
• 卷：18
• 期：20
• 页码：7310-7320
• 全文大小：709 K

文摘

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 IC₅₀ 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.