Total Synthesis of Teixobactin
Total Synthesis of Teixobactin
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DOI：
10.1021/acs.orglett.6b01324
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发表时间：
2016-06-03
期刊：
影响因子：
5.2
通讯作者：
Payne, Richard J.
中科院分区：
文献类型：
--
作者：
Giltrap, Andrew M.;Dowrnan, Luke J.;Payne, Richard J.
首次全合成环状缩肽类天然产物teixobactin。通过固相肽合成实现合成，将不寻常的L-异丙酰亚胺作为适当保护的合成盒，并采用关键的树脂上酯化和溶液相大环内酰胺化。合成的天然产物被证明对一系列革兰氏阳性致病菌具有有效的抗菌活性，包括结核分枝杆菌和耐甲氧西林金黄色葡萄球菌（MRSA）的强毒株。
The first total synthesis of the cyclic depsipeptide natural product teixobactin is described. Synthesis was achieved by solid-phase peptide synthesis, incorporating the unusual 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).