Ping Yang, Wenbo Mao, Jingying Zhang, Yinyin Yang, Fangyan Zhang, Xu Ouyang, Beibei Li, Xiaoyan Wu, Zufang Ba, Kaixin Ran, Yali Tian, Hui Liu, Yun Zhang, Sanhu Gou, Chao Zhong, Jingman Ni
The global issue of antibiotic resistance is increasingly severe, highlighting the urgent necessity for the development of new antibiotics. Brevicidine, a natural cyclic lipopeptide, exhibits remarkable antimicrobial activity against Gram-negative bacteria. In this study, a comprehensive structure-activity relationship of Brevicidine was investigated through 20 newly synthesized cyclic lipopeptide analogs, resulting in the identification of an optimal linear analog 22. The sequence of analog 22 consisted of five d-amino acids and four non-natural amino acid 2,5-diaminovaleric acid (Orn) and conjugated with decanoic acid at N-terminal...
March 15, 2024: European Journal of Medicinal Chemistry