Synthesis and biological evaluation of new enantiomerically pure azole derivatives as inhibitors of Mycobacterium tuberculosis

被引：58

作者：

Castagnolo, Daniele ^{[1
]}

Radi, Marco ^{[1
]}

Dessi, Filippo ^{[1
]}

Manetti, Fabrizio ^{[1
]}

Saddi, Manuela ^{[2
]}

Meleddu, Rita ^{[2
]}

De Logu, Alessandro ^{[2
]}

Botta, Maurizio ^{[1
,3
]}

机构：

[1] Univ Siena, Dipartimento Farm Chim Tecnol, I-53100 Siena, Italy

[2] Univ Cagliari, Sez Microbiol Med, Dipartimento Sci & Tecnol Biomed, I-09123 Cagliari, Italy

[3] Temple Univ, Coll Sci & Technol, Ctr Biotechnol, Sbarro Inst Canc Res & Mol Med, Philadelphia, PA 19122 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 08期

关键词：

Azole; Click chemistry; Tuberculosis; Antifungal agents; CYTOCHROME-P450; ANTIFUNGALS; BINDING;

D O I：

10.1016/j.bmcl.2009.02.101

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel enantiomerically pure azole derivatives was synthesized. The new compounds, bearing both an imidazole as well as a triazole moiety, were evaluated as antimycobacterial agents. One of them proved to have activity against Mycobaterium tuberculosis comparable to those of the classical antibacte-rial/antifungal drugs Econazole and Clotrimazole. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2203 / 2205

页数：3

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