European journal of medicinal chemistry · 2022
Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
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Zhai Hongjin, Luo Chunying, Yang Pu, Zhang Shuo, Wang Huanhuan, Cao Yaquan, Yang Yingxue, Liu Haoyue, Kong Xiaoyan, Arhema Frejat Firas Obald, Ren Changzhong, Shi Xiufang, Wu Chunli
Аннотация
With the increasing incidence of antibiotic resistance, there is an urgent need to develop new antibiotics with excellent activity against drug-resistant bacteria. Three novel series of tylosin semisynthetic derivatives were designed, synthesized and evaluated for their antibacterial activities against various Gram-positive and Gram-negative bacteria. Among these derivatives, compound C-2 demonstrated potent antibacterial activity against both gram-positive and gram negative bacteria, and non mutagenic. More importantly, compound C-2 displayed high antimicrobial potency against Gram-positive bacteria in a murine model, and was found to be more efficient than tildipirosin. Thus, compound C-2 had great potential as a promising lead compound for the treatment of bacterial infection.