Journal
JOURNAL OF ANTIBIOTICS
Volume 72, Issue 2, Pages 118-121Publisher
JAPAN ANTIBIOTICS RESEARCH ASSOC
DOI: 10.1038/s41429-018-0121-4
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Funding
- National Natural Science Foundation of China [81361138018, 21572179]
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Thirteen azolylthioacetamides was synthesized and characterized. Biological activity assays with M beta Ls 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 mu M. 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.
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