Teixobactin, a cyclic-peptide antibiotic, destroys the cell walls of Gram-positive bacteria. It is therefore difficult for bacteria such as meticillin-resistant Staphylococcus aureus to develop resistance to it. Many scholars have studied the structure-activity relationship (SAR) of teixobactin. After reviewing the reports related to the discovery, structure, total synthesis and SAR of teixobactin, we found that the total synthesis of teixobactin was very difficult. The N-terminal methyl modification, ester bond and allo-End were unnecessary for the activity, the configuration of amino acids at the positions 1, 4, 5 and 8 could greatly influence the antibacterial activity, and the substitution of the amino acids at the 3, 4, 9 and 10 positions by Lys could retain the antibacterial activity.%环肽抗生素替索巴丁(teixobactin)通过破坏革兰阳性菌的细胞壁杀灭细菌,因而耐甲氧西林金黄色葡萄球菌等很难对其产生出耐药性.众多学者对该药的构效关系进行了研究.笔者查阅国内外相关报道,从其发现、结构、全合成情况及构效关系等方面汇总后发现,替索巴丁的全合成非常困难,N端甲基修饰、酯键及非天然氨基酸allo-End等为非必要结构,1、4、5、8位氨基酸的构型对抗菌活性影响较大,3、4、9、10位氨基酸被Lys替代后能较大程度地保留抗菌能力.
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