Triazole-Linked Glycolipids Enhance the Susceptibility of MRSA to β-Lactam Antibiotics.
Xi-Le Hu, Dan Li, Lei Shao, Xiaojing Dong, Xiao-Peng He, Guo-Rong Chen, Daijie Chen
Author Information
Xi-Le Hu: Key Laboratory for Advanced Materials & Institute of Fine Chemicals, East China University of Science and Technology , 130 Meilong Road, Shanghai 200237, PR China.
Dan Li: State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry , Shanghai 200040, PR China.
Lei Shao: State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry , Shanghai 200040, PR China.
Xiaojing Dong: State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry , Shanghai 200040, PR China.
Xiao-Peng He: Key Laboratory for Advanced Materials & Institute of Fine Chemicals, East China University of Science and Technology , 130 Meilong Road, Shanghai 200237, PR China.
Guo-Rong Chen: Key Laboratory for Advanced Materials & Institute of Fine Chemicals, East China University of Science and Technology , 130 Meilong Road, Shanghai 200237, PR China.
Daijie Chen: State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry , Shanghai 200040, PR China.
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 β-lactam antibiotics. We determine that the glycolipids can suppress the minimal inhibitory concentration of a number of ineffective β-lactams, upward of 256-fold, for methicillin-resistant Staphylococuss aureus (MRSA). The mechanism of action has been preliminarily probed and discussed.
