Facilely Accessible Quinoline Derivatives as Potent Antibacterial Agents

Publication date: Available online 22 May 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Peng Teng, Chunhui Li, Zhong Peng, Anne Marie Vanderschouw, Alekhya Nimmagadda, Ma Su, Yaqiong Li, Xingmin Sun, Jianfeng Cai
Quinoline compounds have been extensively explored as anti-malaria and anti-cancer agents for decades and show profound functional bioactivities, however, the studies of these compounds in other medicinal fields have lagged dramatically. In this study, we report the development of a series of facilely accessible quinoline derivatives that display potent antibacterial activity against a panel of multidrug-resistant Gram-positive bacterial strains, especially C. difficile. We also demonstrated that these molecules are effective in vivo against C. difficile. These results revealed that these types of quinoline compounds could serve as prototypes for the development of an appealing class of antibiotic agents used to combat Gram-positive drug-resistant bacterial strains, including C. difficile.

Graphical abstract

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