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新型对映体纯唑类衍生物作为结核分枝杆菌抑制剂的合成及生物学评价

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

作者信息

Castagnolo Daniele, Radi Marco, Dessì Filippo, Manetti Fabrizio, Saddi Manuela, Meleddu Rita, De Logu Alessandro, Botta Maurizio

机构信息

Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Siena, Italy.

出版信息

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2203-5. doi: 10.1016/j.bmcl.2009.02.101. Epub 2009 Feb 28.

DOI:10.1016/j.bmcl.2009.02.101
PMID:19299129
Abstract

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 antibacterial/antifungal drugs Econazole and Clotrimazole.

摘要

合成了一系列新型对映体纯的唑类衍生物。这些带有咪唑和三唑部分的新化合物被评估为抗分枝杆菌剂。其中一种化合物对结核分枝杆菌的活性被证明与经典抗菌/抗真菌药物益康唑和克霉唑相当。

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