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

被引：57
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.
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收藏
页码：2203 / 2205
页数：3
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