Synthesis and evaluation of monoamidoxime derivatives: Toward new antileishmanial compounds

被引：25

作者：

Paloque, Lucie ^{[4
]}

Bouhlel, Ahlem ^{[1
,2
,3
]}

Curti, Christophe ^{[1
,2
,3
]}

Dumetre, Aurelien ^{[4
]}

Verhaeghe, Pierre ^{[1
,2
,3
]}

Azas, Nadine ^{[4
]}

Vanelle, Patrice ^{[1
,2
,3
]}

机构：

[1] Univ Aix Marseille 1, Fac Pharm, CNRS, Lab Chim Provence,LPCR,UMR 6264, F-13385 Marseille 05, France

[2] Univ Aix Marseille 2, Fac Pharm, CNRS, Lab Chim Provence,LPCR,UMR 6264, F-13385 Marseille 05, France

[3] Univ Aix Marseille 3, Fac Pharm, CNRS, Lab Chim Provence,LPCR,UMR 6264, F-13385 Marseille 05, France

[4] Univ Aix Marseille 2, Fac Pharm, UMR Relat Hote Parasites MD3, F-13385 Marseille 05, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 07期

关键词：

Manganese(III) acetate; Amidoxime; Leishmania donovani; Anti-infectious; HUMAN AFRICAN TRYPANOSOMIASIS; PENTAMIDINE; CHEMOTHERAPY; MODELS; DRUGS;

D O I：

10.1016/j.ejmech.2011.04.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of monoamidoxime derivatives was synthesized using manganese(III) acetate by microwave irradiation. Several amidoximes (27-31, 33, 38) showed valuable in vitro activities toward Leishmania donovani promastigotes, exhibiting IC50 values between 5.21 and 7.89 mu M. In parallel, the cytotoxicity of these compounds was evaluated on murine J774A.1 cells, revealing the corresponding selectivity index (SI). Among the 13 tested compounds, 4 monoamidoximes (27-30) exhibited an SI more than 20 times better than pentamidine. Moreover, monoamidoxime 28 (4-[5-Benzyl-3-(4-fluorophenylsulfonyl)-5-methyl-4,5-dihydrofuran-2-yl]-N'-hydroxybenzimidamide) is 40 times more selective than pentamidine, and 1.6 times more than amphotericin B, used as reference drug compounds. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：2984 / 2991

页数：8

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