Azolylthioacetamides as potential inhibitors of New Delhi metallo-β-lactamase-1 (NDM-1)

Thirteen azolylthioacetamides was synthesized and characterized. Biological activity assays with MβLs revealed that all of these compounds (except 3 and 6) gained exhibited inhibitory activity on NDM-1, with an IC50 value ranging from 3.8 to 26.4 μM. Inhibitors 11 and 13, in combination with cefazolin, resulted in a four-fold decrease in MIC of the antibiotic against Escherichia coli cells expressing NDM-1. Docking studies revealed that the inhibitors 7, 9, and 13 bound to active site of NDM-1.