Recent Advances in the Discovery of Metallo-β--Lactamase Inhibitors for β-lactam Antibiotic-Resistant Reversing Agents
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.
Keywords: Antibiotic, β-lactam, inhibitor, metallo-β-lactamase, resistant and zinc enzyme.
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