β-lactam/β-lactamase inhibitor combinations: an update,RSC Medicinal Chemistry

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β-lactam/β-lactamase inhibitor combinations: an update
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-08-17 00:00:00 , DOI: 10.1039/c8md00342d
Kamaleddin H M E Tehrani ₁ , Nathaniel I Martin _{1,

2}

Affiliation

Antibiotic resistance caused by β-lactamase production continues to present a growing challenge to the efficacy of β-lactams and their role as the most important class of clinically used antibiotics. In response to this threat however, only a handful of β-lactamase inhibitors have been introduced to the market over the past thirty years. The first-generation β-lactamase inhibitors (clavulanic acid, sulbactam and tazobactam) are all β-lactam derivatives and work primarily by inactivating class A and some class C serine β-lactamases. The newer generations of β-lactamase inhibitors including avibactam and vaborbactam are based on non-β-lactam structures and their spectrum of inhibition is extended to KPC as an important class A carbapenemase. Despite these advances several class D and virtually all important class B β-lactamases are resistant to existing inhibitors. The present review provides an overview of recent FDA-approved β-lactam/β-lactamase inhibitor combinations as well as an update on research efforts aimed at the discovery and development of novel β-lactamase inhibitors.

中文翻译：

β-内酰胺/β-内酰胺酶抑制剂组合：更新

由 β-内酰胺酶产生引起的抗生素耐药性继续对 β-内酰胺的功效及其作为临床使用的最重要抗生素类别的作用提出越来越大的挑战。然而，为了应对这一威胁，在过去三十年中，只有少数β-内酰胺酶抑制剂被引入市场。第一代β-内酰胺酶抑制剂（克拉维酸、舒巴坦和他唑巴坦）都是β-内酰胺衍生物，主要通过灭活A类和部分C类丝氨酸β-内酰胺酶发挥作用。包括阿维巴坦和伐波巴坦在内的新一代β-内酰胺酶抑制剂基于非β-内酰胺结构，其抑制谱扩展到KPC作为重要的A类碳青霉烯酶。尽管取得了这些进展，但几种 D 类和几乎所有重要的 B 类 β-内酰胺酶都对现有抑制剂具有耐药性。本综述概述了 FDA 最近批准的 β-内酰胺/β-内酰胺酶抑制剂组合，以及旨在发现和开发新型 β-内酰胺酶抑制剂的研究工作的最新情况。

更新日期：2018-08-17

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