Synthesis and Inhibitory Activity of Oxazolethioacetamides against Metallo‐β‐Lactamase.

The metallo‐β‐lactamases (MβLs) produced by pathogens has issued a challenge to the treatment of bacterial infections worldwide. A number of oxazolethioacetamides were designed and synthesized as potential MβLs inhibitors. Most of the compounds displayed inhibitory activity against MβL L1 with an IC50 value range of 0.19–0.38 μM. The fluorine substituted compounds also inhibited VIM‐2 with IC50 value of 2.1 to 6.8 μM. Molecule Docking showed the style and position of electron withdrawing groups played important role between the oxazolethioacetamides and MβLs. [ABSTRACT FROM AUTHOR]