文献类型：期刊文献

英文题名：Triazole-Linked Glycolipids Enhance the Susceptibility of MRSA to β-Lactam Antibiotics

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

年份：2015

卷号：6

期号：7

起止页码：793

外文期刊名：ACS MEDICINAL CHEMISTRY LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000357965900012)】；

基金：We thank the 973 project (2013CB733700), the National Natural Science Foundation of China (81373310), and the Ministry of Science and Technology of China (2014ZX09507009-025). Zhonglei Li is thanked for his aid in antimicrobial tests. The Institute of Antibiotics of Huashan Hospital of Fudan University is warmly thanked for kindly providing the clinical isolates. Bing Ni at ECNU is thanked for help in SEM imaging.

语种：英文

外文关键词：Triazolyl glycolipid; click reaction; beta-lactams; MRSA; superbacteria

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.