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MurD inhibitors as antibacterial agents: a review
Chemical Papers ( IF 2.1 ) Pub Date : 2020-01-13 , DOI: 10.1007/s11696-020-01057-w
Mohammed Afzal Azam , Srikanth Jupudi

Peptidoglycan is an essential component of the bacterial cell wall and is required for the survival of bacteria. ATP-dependent MurC–F ligases are responsible for the early stages of peptidoglycan biosynthesis. Second in the series, MurD catalyzes the addition of d-glutamic acid to UDP-MurNAc-l-Ala which involves acyl-phosphate and tetrahedral intermediates. Due to its high specificity for d-glutamic acid substrate and its absence in mammalian cells, MurD is considered as an attractive target for the design of novel antibacterial agents. Several MurD inhibitors have been designed and tested for their activity. These include phosphinates, N-acetylmuramic acids, pulvinones, phosphinodipeptide, cyclic nonapeptides, macrocyclic compounds, benzene-1,3-dicarboxylic acid, naphthalene sulphonamides, 2-thioxothiazolidin-4-ones, benzylidene-2,4-thiazolidindiones, etc. In the present review, an updated status of MurD enzyme inhibitors is presented which will serve as a useful source of structural information and may be utilized for the design of potent inhibitors against this enzyme.

中文翻译:

MurD抑制剂作为抗菌剂:综述

肽聚糖是细菌细胞壁的重要组成部分,是细菌生存所必需的。ATP依赖性MurC-F连接酶负责肽聚糖生物合成的早期阶段。在该系列的第二篇文章中,MurD催化将d-谷氨酸添加到UDP-MurNAc-1-Ala中,后者涉及酰基磷酸酯和四面体中间体。由于其对d-谷氨酸底物的高度特异性以及在哺乳动物细胞中的缺失,MurD被认为是设计新型抗菌剂的诱人靶标。已经设计和测试了几种MurD抑制剂的活性。这些包括次膦酸盐,N-乙酰基山酰胺酸,pulvinones,膦二肽,环状九肽,大环化合物,苯-1,3-二羧酸,萘磺酰胺,2-硫代噻唑烷酮-4-酮,亚苄基-2,4-噻唑烷二酮等。介绍了MurD酶抑制剂的最新状态,它将作为有用的结构信息来源,并可用于设计针对该酶的有效抑制剂。
更新日期:2020-01-13
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