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新千年的β-内酰胺类抗生素。第一部分:单环β-内酰胺类抗生素和碳青霉烯类抗生素。

Beta-lactams in the new millennium. Part-I: monobactams and carbapenems.

作者信息

Singh G S

机构信息

Chemistry Department, University of Botswana, Private Bag 0022, Gaborone, Botswana.

出版信息

Mini Rev Med Chem. 2004 Jan;4(1):69-92. doi: 10.2174/1389557043487501.

Abstract

Beta-lactam ring-containing compounds such as penicillins, ampicillin, amoxicillin, cephalosporins and carbapenem are among the most famous antibiotics. This article reviews the recent developments in the study of such compounds. The introductory paragraph, which highlights the significance of the subject and cites most of the leading references of the previous century, is followed by an overview of beta-lactams and some novel methodologies for the synthesis of bi-, tri- and polycyclic derivatives. The rest of the sections deal with design, synthesis and biological activity of monobactams and carbapenems. Many of them have potential antibacterial activity, even against some resistant strains, and enzyme inhibitory activity.

摘要

含β-内酰胺环的化合物,如青霉素、氨苄青霉素、阿莫西林、头孢菌素和碳青霉烯,是最著名的抗生素之一。本文综述了此类化合物研究的最新进展。引言部分强调了该主题的重要性,并引用了上世纪的大部分主要参考文献,随后是β-内酰胺的概述以及一些合成双环、三环和多环衍生物的新方法。其余部分涉及单环β-内酰胺和碳青霉烯的设计、合成及生物活性。它们中的许多具有潜在的抗菌活性,甚至对一些耐药菌株也有效,并且具有酶抑制活性。

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