Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA

被引：84

作者：

Bachelier, Anke

Mayer, Ralf

Klein, Christian D. ^{[1
]}

机构：

[1] Univ Saarland, Saarbrucken, Germany

[2] Univ Bonn, D-5300 Bonn, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 21期

关键词：

sesquiterpene lactones; antibiotic; peptidoglycan biosynthesis; MurA; structure-activity relationships;

D O I：

10.1016/j.bmcl.2006.08.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the identification of the sesquiterpene lactones cnicin and cynaropicrin as potent, irreversible inhibitors of the bacterial enzyme MurA. They covalently bind to the thiol group of Cys115. Judging from the structure-activity relationships, we conclude that the unsaturated ester side chain of cynaropicrin and cnicin is of particular importance for the inhibition of MurA. These results provide evidence that MurA is a target protein of SLs with a probably high relevance for their known antibacterial effect. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：5605 / 5609

页数：5

共 23 条

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