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设计、合成及一系列新型 2-氧代异头孢烯类化合物的抗菌活性。

Design, synthesis and antibacterial activities of a series of new 2-oxaisocephems.

机构信息

Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.

出版信息

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5293-6. doi: 10.1016/j.bmcl.2012.06.040. Epub 2012 Jun 23.

DOI:10.1016/j.bmcl.2012.06.040
PMID:22795329
Abstract

A series of 2-oxaisocephems with a thio-substituted methyl group at the 3-position and a [2-(5-amino-1,2,4-thiadizol-3-yl)-2-(Z)-alkoxyimino]acetamido moiety at 7-position were synthesized and tested for their antibacterial activities. The analogs 17c and 17f have well-balanced potency and significantly enhanced activity as compared with the reference compound ceftazidime.

摘要

一系列 2-氧代异头孢烯类化合物，其 3-位具有硫取代甲基，7-位具有 [2-(5-氨基-1,2,4-噻二唑-3-基)-2-(Z)-烷氧基亚氨基]乙酰胺基部分，被合成并测试了它们的抗菌活性。与参比化合物头孢他啶相比，类似物 17c 和 17f 具有平衡的效力和显著增强的活性。

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