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作为新型细菌烯酰-ACP还原酶FabK抑制剂的苯基咪唑衍生物

Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK.

作者信息

Kitagawa Hideo, Ozawa Tomohiro, Takahata Sho, Iida Maiko

机构信息

Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Meiji Seika Kaisha Ltd, Yokohama, Japan.

出版信息

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4982-6. doi: 10.1016/j.bmcl.2007.06.040. Epub 2007 Jun 14.

DOI:10.1016/j.bmcl.2007.06.040
PMID:17600706
Abstract

Novel FabK inhibitors with antibacterial activity against Streptococcus pneumoniae were synthesized and evaluated. Through SAR studies of our initial hit compound 2-(1H-benz[d]imidazol-2-ylthio)-N-(6-methoxycarbonylbenzo[d]thiazol-2-yl)acetamide, a series of novel phenylimidazole derivatives were discovered as potent FabK inhibitors.

摘要

合成并评估了对肺炎链球菌具有抗菌活性的新型FabK抑制剂。通过对我们最初发现的活性化合物2-(1H-苯并[d]咪唑-2-基硫代)-N-(6-甲氧基羰基苯并[d]噻唑-2-基)乙酰胺进行构效关系研究，发现了一系列新型苯并咪唑衍生物作为有效的FabK抑制剂。

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