一种基于机制的 GlcNAc 启发的环磷醇抑制剂，可使肽聚糖回收酶 NagZ 失活，从而逆转铜绿假单胞菌对β-内酰胺类抗生素的耐药性。
A mechanism-based GlcNAc-inspired cyclophellitol inactivator of the peptidoglycan recycling enzyme NagZ reverses resistance to β-lactams in Pseudomonas aeruginosa.
机构信息
School of Molecular Sciences, University of Western Australia, Crawley, WA 6009, Australia.
Department of Microbiology, University of Manitoba, Winnipeg, Manitoba R3T2N2, Canada.
出版信息
Chem Commun (Camb). 2018 Sep 25;54(75):10630-10633. doi: 10.1039/c8cc05281f. Epub 2018 Sep 4.
PMID:30178799
Abstract
The development of a potent mechanism-based inactivator of NagZ, an enzyme critical to the production of inducible AmpC β-lactamase in Gram-negative bacteria, is presented. This inactivator significantly reduces MIC values for important β-lactams against a clinically relevant strain of Pseudomonas aeruginosa.
摘要
本文介绍了一种强效的 NagZ 机制失活剂的开发，NagZ 是革兰氏阴性菌中诱导型 AmpC β-内酰胺酶产生的关键酶。该失活剂显著降低了临床相关铜绿假单胞菌菌株对重要β-内酰胺类抗生素的 MIC 值。
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