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

被引：11

作者：

Liu, Xiao-Long ^{[1
,2
]}

Xiang, Yang ^{[1
,3
]}

Chen, Cheng ^{[1
]}

Yang, Ke-Wu ^{[1
]}

机构：

[1] Northwest Univ, Coll Chem & Mat Sci, Key Lab Synthet & Nat Funct Mol Chem, Chem Biol Innovat Lab,Minist Educ, Xian 710127, Shaanxi, Peoples R China

[2] Yanan Univ, Med Coll, Yanan 716000, Peoples R China

[3] Yanan Univ, Coll Phys Educ, Yanan 716000, Peoples R China

来源：

JOURNAL OF ANTIBIOTICS | 2019年 / 72卷 / 02期

基金：

中国国家自然科学基金;

关键词：

METALLO-BETA-LACTAMASE; SCAFFOLD; TRIAZOLYLTHIOACETAMIDE; INSIGHTS;

D O I：

10.1038/s41429-018-0121-4

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

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.

引用

收藏

页码：118 / 121

页数：4

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