Total synthesis and structure-activity relationship of cyclic peptide antibiotic teixobactin:research advances

VernacularTitle:环肽抗生素替索巴丁全合成及构效关系研究进展
Author: Chang-Bing LI ¹ ; Hong-Li LIAO ; He JIANG
Author Information

1. 成都医学院药学院
Keywords: cyclic peptide antibiotics; teixobactin; Gram-positive bacteria; solid phase peptide synthesis
From: Journal of International Pharmaceutical Research 2018;45(8):582-587
CountryChina
Language:Chinese
Abstract: 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.