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|Title:||Targeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors||Authors:||Brindisi, Margherita
DE LUCA, Filomena
Docquier, JEAN DENIS
|Keywords:||Antibiotic resistance; docking; metallo-β-lactamase||Issue Date:||2016||Project:||None||Journal:||JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY||Abstract:||
Metallo-β-lactamases (MBLs) represent one of the most important and widespread mechanisms of resistance to β-lactam antibiotics (including the life-saving carbapenems), against which no clinically useful inhibitors are currently available. We report herein a structure-based high-throughput docking (HTD) campaign on three clinically-relevant acquired MBLs (IMP-1, NDM-1 and VIM-2). The initial hit NF1810 (1) was optimized providing the broad-spectrum inhibitor 3i, which is able to potentiate the in vitro activity of cefoxitin on a VIM-2-producing E. coli strain.
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