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

Liu Xiao-Long; Xiang Yang; Chen Cheng; Yang Ke-Wu

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

机译：紫醇硫代乙酰胺作为新德里金属 - β-乳酰胺酶-1（NDM-1）的潜在抑制剂

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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.

机译：合成并表征了13个紫醇硫代乙酰胺。具有MβLS的生物活性测定揭示了所有这些化合物（3和6）在NDM-1上获得了抑制活性，其IC50值范围为3.8至26.4μm。抑制剂11和13，与Cefazolin组合，导致抗生素的MIC减少对表达NDM-1的大肠杆菌细胞的抗生素的降低。对接研究表明，抑制剂7,9和13结合到NDM-1的活性位点。

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《The Journal of Antibiotics: An International Journal》 |2019年第2期|共4页
作者
Liu Xiao-Long; Xiang Yang; Chen Cheng; Yang Ke-Wu;
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作者单位

Northwest Univ Coll Chem &

Mat Sci Key Lab Synthet &

Nat Funct Mol Chem Chem Biol Innovat Lab;

Northwest Univ Coll Chem &

Mat Sci Key Lab Synthet &

Nat Funct Mol Chem Chem Biol Innovat Lab;

Northwest Univ Coll Chem &

Mat Sci Key Lab Synthet &

Nat Funct Mol Chem Chem Biol Innovat Lab;

Northwest Univ Coll Chem &

Mat Sci Key Lab Synthet &

Nat Funct Mol Chem Chem Biol Innovat Lab;

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正文语种 eng
中图分类药学;
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1. Azolylthioacetamides as potential inhibitors of New Delhi metallo-beta-lactamase-1 (NDM-1) [J] . Liu Xiao-Long, Xiang Yang, Chen Cheng, The Journal of Antibiotics: An International Journal . 2019,第2期

机译：紫醇硫代乙酰胺作为新德里金属 - β-乳酰胺酶-1（NDM-1）的潜在抑制剂
2. 3-Bromopyruvate as a potent covalently reversible inhibitor of New Delhi metallo-beta-lactamase-1 (NDM-1) [J] . Kang Peng-Wei, Su Jian-Peng, Sun Le-Yun, European journal of pharmaceutical sciences . 2020,第期

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

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