Triazole-Linked Glycolipids Enhance the Susceptibility of MRSA to β-Lactam Antibiotics

被引：26

作者：

Hu, Xi-Le ^{[1
,2
]}

Li, Dan ^{[3
]}

Shao, Lei ^{[3
]}

Dong, Xiaojing ^{[3
]}

He, Xiao-Peng ^{[1
,2
]}

Chen, Guo-Rong ^{[1
,2
]}

Chen, Daijie ^{[3
]}

机构：

[1] E China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China

[2] E China Univ Sci & Technol, Inst Fine Chem, Shanghai 200237, Peoples R China

[3] China State Inst Pharmaceut Ind, Shanghai Inst Pharmaceut Ind, State Key Lab New Drug & Pharmaceut Proc, Shanghai 200040, Peoples R China

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2015年 / 6卷 / 07期

基金：

中国国家自然科学基金;

关键词：

Triazolyl glycolipid; click reaction; beta-lactams; MRSA; superbacteria; CLICK CHEMISTRY; STAPHYLOCOCCUS-AUREUS; RESISTANCE; PENICILLIN; AZIDES;

D O I：

10.1021/acsmedchemlett.5b00142

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We show here that a series of triazolyl glycolipid derivatives modularly synthesized by a "click" reaction have the ability to increase the susceptibility of a drug-resistant bacterium to beta-lactam antibiotics. We determine that the glycolipids can suppress the minimal inhibitory concentration of a number of ineffective beta-lactams, upward of 256-fold, for methicillin-resistant Staphylococuss aureus (MRSA). The mechanism of action has been preliminarily probed and discussed.

引用

页码：793 / 797

页数：5

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