The Development of New Small-Molecule Inhibitors Targeting Bacterial Metallo-β-lactamases

Title:The Development of New Small-Molecule Inhibitors Targeting Bacterial Metallo-β-lactamases

Volume: 18 Issue: 10

Author(s): Ping Wang, Jing Cheng, Cong-Cong Liu, Kai Tang, Feng Xu, Zhiqiang Yu, Bin Yu*Junbiao Chang*

Affiliation:

• Co-Innovation Center of Henan Province for New Drug R & D and Preclinical Safety, Zhengzhou 450001,China

• Co-Innovation Center of Henan Province for New Drug R & D and Preclinical Safety, Zhengzhou 450001,China

Keywords: Metallo-β-lactamases, thiol derivatives, dicarboxylic acid derivatives, cyclic Boronates, triazoles, natural products, peptide inhibitors.

Abstract: Metallo-β-lactamases (MBLs) are a family of Zn(II)-dependent enzymes that can hydrolyze almost all β-lactam antibiotics. Horizontal transfer of the genes encoding MBLs among Gram-negative bacteria pathogens has led to the emergence of extensively drug-resistant pathogens, which now represent a major threat to human health. As there is not to date yet a clinically available MBL inhibitor, the discovery of new MBL inhibitors has great urgency. This review highlights the recent developments in the discovery of small-molecule MBL inhibitors.

Cite this article as:

Wang Ping, Cheng Jing, Liu Cong-Cong, Tang Kai, Xu Feng, Yu Zhiqiang, Yu Bin*, Chang Junbiao*, The Development of New Small-Molecule Inhibitors Targeting Bacterial Metallo-β-lactamases, Current Topics in Medicinal Chemistry 2018; 18 (10) . https://dx.doi.org/10.2174/1568026618666180518101028