Total Synthesis of Teixobactin
详细信息 查看全文
- 作者：Andrew M. Giltrap ; Luke J. Dowman ; Gayathri Nagalingam ; Jessica L. Ochoa ; Roger G. Linington ; Warwick J. Britton ; Richard J. Payne
- 刊名：Organic Letters
- 出版年：2016
- 出版时间：June 3, 2016
- 年：2016
- 卷：18
- 期：11
- 页码：2788-2791
- 全文大小：299K
- 年卷期：0
- ISSN：1523-7052
文摘
The first total synthesis of the cyclic depsipeptide natural product teixobactin is described. Synthesis was achieved by solid-phase peptide synthesis, incorporating the unusual mallcaps">l-allo-enduracididine as a suitably protected synthetic cassette and employing a key on-resin esterification and solution-phase macrolactamization. The synthetic natural product was shown to possess potent antibacterial activity against a range of Gram-positive pathogenic bacteria, including a virulent strain of Mycobacterium tuberculosis and methicillin-resistant Staphylococcus aureus (MRSA).