Department of Chemistry, Fudan University, Shanghai, 200433, P. R. China.
College of Life Science, Fujian Agriculture and Forestry University, Fuzhou, 350002, P. R. China.
Chemistry. 2018 Apr 11;24(21):5406-5422. doi: 10.1002/chem.201704167. Epub 2017 Dec 12.
Bacterial resistance to existing drugs is becoming a serious public health issue, urging extensive search for new antibiotics. Teixobactin, a cyclic depsipeptide discovered in a screen of uncultured bacteria, shows potent activity against all the tested Gram-positive bacteria. Remarkably, no teixobactin-resistant bacterial strain has been obtained despite extensive efforts, highlighting the great potential of teixobactin as a lead compound in the fight against antimicrobial resistance (AMR). This review summarizes recent progresses in the understanding of many aspects of teixobactin, including chemical structure, biological activity, biosynthetic pathway, and mode of action. We also discuss the different synthetic strategies in producing teixobactin and its analogues, and the structure-activity relationship (SAR) studies.
细菌对现有药物的耐药性正成为一个严重的公共卫生问题，促使人们广泛寻找新的抗生素。从未培养的细菌筛选中发现的环缩肽泰妙菌素对所有测试的革兰氏阳性菌均具有很强的活性。值得注意的是，尽管进行了广泛的努力，但仍未获得耐泰妙菌素的细菌菌株，这突出了泰妙菌素作为对抗抗微生物药物耐药性（AMR）的先导化合物的巨大潜力。本文综述了近年来在理解泰妙菌素的许多方面取得的进展，包括化学结构、生物活性、生物合成途径和作用模式。我们还讨论了生产泰妙菌素及其类似物的不同合成策略，以及结构-活性关系（SAR）研究。
