期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 242, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2022.114677
关键词
Serine-?-Lactamase; Metallo-?-Lactamase; Antibiotic resistance; Inhibition mode; Dual -action inhibitors
资金
- Chengdu Science and Technology Bureau, China [2019-YF05-02095-SN]
- Xihua University graduate innovation funds [YCJJ2021104]
The effectiveness of beta-lactam antibiotics is increasingly influenced by serine beta-lactamases (SBLs) and metallo beta-lactamases (MBLs). Developing effective beta-lactamase inhibitors is important to extend the use of beta-lactam antibiotics. Although SBL inhibitors have been approved for clinical use, there are currently no MBL inhibitors or MBL/SBL dual-action inhibitors.
The effectiveness of beta-lactam antibiotics is increasingly influenced by serine beta-lactamases (SBLs) and metallo beta-lactamases (MBLs), which can hydrolyze beta-lactam antibiotics. The development of effective beta-lactamase inhibitors is an important direction to extend use of beta-lactam antibiotics. Although six SBL inhibitors have been approved for clinical use, but no MBL inhibitors or MBL/SBL dual-action inhibitors are available so far. Broadspectrum targeting clinically relevant MBLs and SBLs is currently desirable, while it is not easy to achieve such a purpose owing to structural and mechanistic differences between MBLs and SBLs. In this review, we summarized recent advances of inhibitor chemotypes targeting MBLs and SBLs and their inhibition mechanisms, particularly including lead discovery and structural optimization strategies, with the aim to provide useful information for future efforts to develop new MBL and SBL inhibitors.
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