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