Jin Kang, Po Kathy Hiu Laam, Wang Shengxi, Reuven Jonathan Avraham, Wai Chi Nga, Lau Ho Ting, Chan Ting Ho, Chen Sheng, Li Xuechen
Department of Chemistry, State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Hong Kong Special Administrative Region.
Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong Special Administrative Region.
Bioorg Med Chem. 2017 Sep 15;25(18):4990-4995. doi: 10.1016/j.bmc.2017.04.039. Epub 2017 Apr 29.
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.
收敛性丝氨酸/苏氨酸连接已被用于制备一系列替考拉宁类似物（共28种），以建立替考拉宁的构效关系。对这些合成类似物的抗菌评估揭示了关键氨基酸残基和可修饰的位点。这些研究将为进一步开发具有更高抗菌活性的替考拉宁类似物提供线索。
