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Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives

2022; Elsevier BV; Volume: 238; Linguagem: Inglês

10.1016/j.ejmech.2022.114495

1768-3254

Hongjin Zhai, Chunying Luo, Yang Pu, Shuo Zhang, Huanhuan Wang, Yaquan Cao, Yingxue Yang, Haoyue Liu, Xiaoyan Kong, Firas Obald Arhema Frejat, Changzhong Ren, Xiufang Shi, Chunli Wu,

Synthesis and Biological Evaluation

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.