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咪唑并[1,2-a]吡啶-8-甲酰胺类衍生物的合成及构效关系研究作为新型抗结核药物先导化合物系列。

Synthesis and structure activity relationship of imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead series.

机构信息

Department of Medicinal Chemistry, AstraZeneca India Pvt Ltd, Avishkar, Bellary Road, Hebbal, Bangalore 560024, India.

出版信息

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4996-5001. doi: 10.1016/j.bmcl.2013.06.043. Epub 2013 Jun 24.

Abstract

Imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead were generated by whole cell screening of a focused library against Mycobacterium tuberculosis. Herein, we describe the synthesis and structure activity relationship evaluation of this class of inhibitors and the optimization of physicochemical properties. These are selective inhibitors of Mycobacterium tuberculosis with no activity on either gram positive or gram negative pathogens.

摘要

通过针对结核分枝杆菌的组合文库的全细胞筛选,生成了咪唑并[1,2-a]吡啶-8-甲酰胺类新型抗分枝杆菌先导化合物。本文描述了该类抑制剂的合成和构效关系评价以及理化性质的优化。它们是结核分枝杆菌的选择性抑制剂,对革兰氏阳性或革兰氏阴性病原体均无活性。

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