Recent Advances in the Discovery of Metallo-β--Lactamase Inhibitors for β-lactam Antibiotic-Resistant Reversing Agents

Title:Recent Advances in the Discovery of Metallo-β--Lactamase Inhibitors for β-lactam Antibiotic-Resistant Reversing Agents

Volume: 15 Issue: 7

Author(s): Zhenzhen Guo and Shutao Ma

Affiliation:

Keywords: Antibiotic, β-lactam, inhibitor, metallo-β-lactamase, resistant and zinc enzyme.

Abstract: The overuse of antibiotics which exerts the selective pressure for bacterial pathogens has facilitated the spread of antibiotics’ resistance. Metallo-β-lactamases (MβLs) are zinc enzymes produced by an increasing number of bacterial pathogens. They can readily cleave carbapenems and most other β-lactams that are mainstays of therapy for bacterial infections. MβL-conferred resistance to antibiotics is most worrisome due to MβLs exhibiting very broad-spectrum resistance. Therefore, the bacteria carrying MβLs have recently become a significant clinical threat. No clinically useful MβLs inhibitor has been discovered yet. To address the serious threat to public health posed by the MβL-conferred resistance to antibiotics, novel effective MβL inhibitors are urgently needed. This review mainly describes various MβL inhibitors, giving special attention to their antibacterial activity, mechanisms of action, structure-activity relationships and synergetic effect with clinically available antibiotics.

Cite this article as:

Guo Zhenzhen and Ma Shutao, Recent Advances in the Discovery of Metallo-β--Lactamase Inhibitors for β-lactam Antibiotic-Resistant Reversing Agents, Current Drug Targets 2014; 15 (7) . https://dx.doi.org/10.2174/1389450115666140326094504