查看文章

Captopril is a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC₅₀ value of 7.9 μM. It is composed of two units: a 3-mercapto-2-methylpropanoyl fragment and a proline residue. In this study, we synthesized simple amide derivatives of 3-mercapto-2-methylpropanoic acid, and then tested them as NDM-1 inhibitors in order to identify the pharmacophore for NDM-1 inhibition. We found that the lead compound 22 had an IC₅₀ value of 1.0 μM. Further structure simplification provided compounds 31 and 32, which had IC₅₀ values of 15 and 10 μM, respectively. As compound 32 is a clinically used antidote for metal poisoning, it has great potential to be repurposed to treat bacterial infections.