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一系列对耐甲氧西林金黄色葡萄球菌具有活性的1-碳-1-去硫头孢烯的发现及其构效关系

Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.

作者信息

Ternansky R J, Draheim S E, Pike A J, Bell F W, West S J, Jordan C L, Wu C Y, Preston D A, Albron W, Kasher J S

机构信息

Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.

出版信息

J Med Chem. 1993 Jul 9;36(14):1971-6. doi: 10.1021/jm00066a006.

Abstract

The synthesis and antimicrobial activity of several new 1-carba-1-dethiacephalosporins is described. The discovery of unique activity of some of the analogues against methicillin-resistant Staphylococcus aureus led to the development of a structure-activity relationship designed to optimize this activity. The results of this investigation along with the pharmacokinetic characteristics of select compounds are described.

摘要

描述了几种新型1-碳-1-去硫头孢菌素的合成及其抗菌活性。一些类似物对耐甲氧西林金黄色葡萄球菌具有独特活性的发现,促使人们建立了一种构效关系以优化这种活性。本文介绍了该研究结果以及所选化合物的药代动力学特征。

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