Department of Chemistry, State Key Lab of Synthetic Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong, China.
Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China.
Nat Commun. 2016 Aug 3;7:12394. doi: 10.1038/ncomms12394.
To cope with the global bacterial multidrug resistance, scientific communities have devoted significant efforts to develop novel antibiotics, particularly those with new modes of actions. Teixobactin, recently isolated from uncultured bacteria, is considered as a promising first-in-class drug candidate for clinical development. Herein, we report its total synthesis by a highly convergent Ser ligation approach and this strategy allows us to prepare several analogues of the natural product.
为应对全球范围内的细菌多重耐药性问题，科学界投入大量精力研发新型抗生素，特别是具有新型作用机制的抗生素。最近从未培养的细菌中分离出的 Teixobactin 被认为是一种很有前途的临床开发的首创类药物候选物。在此，我们通过高度会聚的 Ser 连接方法报告了其全合成，该策略使我们能够制备几种天然产物的类似物。
