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Recent advances in the development of β-lactamase inhibitors.
Journal of Microbiology ( IF 3 ) Pub Date : 2020-07-27 , DOI: 10.1007/s12275-020-0285-z
Shivakumar S Jalde 1 , Hyun Kyung Choi 1
Affiliation  

β-Lactam antibiotics are the most commonly prescribed antibiotics worldwide; however, antimicrobial resistance (AMR) is a global challenge. The β-lactam resistance in Gram-negative bacteria is due to the production of β-lactamases, including extended-spectrum β-lactamases, metallo-β-lactamases, and carbapenem-hydrolyzing class D β-lactamases. To restore the efficacy of BLAs, the most successful strategy is to use them in combination with β-lactamase inhibitors (BLI). Here we review the medically relevant β-lactamase families and penicillins, diazabicyclooctanes, boronic acids, and novel chemical scaffold-based BLIs, in particular approved and under clinical development.

中文翻译:

β-内酰胺酶抑制剂的最新进展。

β-内酰胺抗生素是世界上最常用的处方抗生素。但是,抗菌素耐药性(AMR)是一个全球性挑战。革兰氏阴性细菌对β-内酰胺的耐药性是由于产生了β-内酰胺酶,包括广谱β-内酰胺酶,金属β-内酰胺酶和碳青霉烯水解的D类β-内酰胺酶。为了恢复BLA的功效,最成功的策略是将它们与β-内酰胺酶抑制剂(BLI)结合使用。在这里,我们回顾医学上相关的β-内酰胺酶家族和青霉素,二氮杂双环辛烷,硼酸和新型基于化学支架的BLI,尤其是已获批准并正在临床开发中。
更新日期:2020-07-27
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