Synthesis and structure-activity relationship of teixobactin analogues via convergent Ser ligation
Synthesis and structure-activity relationship of teixobactin analogues via convergent Ser ligation
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DOI：
10.1016/j.bmc.2017.04.039
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发表时间：
2017-09-15
影响因子：
3.5
通讯作者：
Li, Xuechen
中科院分区：
文献类型：
--
作者：
Jin, Kang;Po, Kathy Hiu Laam;Li, Xuechen
采用Ser/Thr聚合连接的方法合成了一系列teixobactin类似物(共28个)，建立了teixobactin的构效关系。对这些合成类似物的抗菌评估揭示了关键的氨基酸残基和可耐受的修饰部位。这些研究将为进一步开发具有更好的抗菌活性的teixobactin类似物提供线索。(C)2017爱思唯尔有限公司。保留所有权利。
Convergent Ser/Thr ligation has been used to prepare a series of teixobactin analogues (28 in total) to establish a structure-activity relationship of teixobactin. anti-bacterial evaluations of these synthetic analogues have revealed the critical amino acid residues and the sites tolerable of modifications. These studies will shed lights on the further development of teixobactin analogues with improved antibacterial activities. (C) 2017 Elsevier Ltd. All rights reserved.