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
收藏
页码：793 / 797
页数：5
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