唑基硫代乙酰胺作为新型德里金属-β-内酰胺酶-1（NDM-1）的潜在抑制剂。
Azolylthioacetamides as potential inhibitors of New Delhi metallo-β-lactamase-1 (NDM-1).
机构信息
Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education, Chemical Biology Innovation Laboratory, College of Chemistry and Materials Science, Northwest University, Xi'an, 710127, P. R. China.
Medical College, Yan'an University, Yan'an, 716000, P. R. China.
出版信息
J Antibiot (Tokyo). 2019 Feb;72(2):118-121. doi: 10.1038/s41429-018-0121-4. Epub 2018 Nov 19.
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 IC 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.
合成并表征了 13 种唑基硫代乙酰胺。对 MβLs 的生物活性测定表明，除 3 和 6 外，所有这些化合物都对 NDM-1 表现出抑制活性，IC 值范围为 3.8 至 26.4μM。抑制剂 11 和 13 与头孢唑林联合使用，使表达 NDM-1 的大肠杆菌细胞对抗生素的 MIC 值降低了四倍。对接研究表明，抑制剂 7、9 和 13 与 NDM-1 的活性位点结合。
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