Design of novel antimicrobial peptide dimer analogues with enhanced antimicrobial activity in vitro and in vivo by intermolecular triazole bridge strategy

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• 作者：Beijun Liu^a ; ^b ; ^{liubj12@lzu.edu.cn} ; Haifeng Huang^c ; Zhibin Yang^d ; Beiyin Liu^e ; Sanhu Gou^a ; Chao Zhong^b ; Xiufeng Han^b ; Yun Zhang^b ; Jingman Ni^a ; ^b ; ^{nijm@lzu.edu.cn} ; Rui Wang^a ; ^{wangrui@lzu.edu.cn}
• 关键词：Click chemistry ; Dimer analogues ; Antimicrobial activity ; α Helical structure ; Drug resistance
• 刊名：Peptides
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：88
• 期：Complete
• 页码：115-125
• 全文大小：2122 K
• 卷排序：88

文摘

A series of side-chain hybrid dimer peptides were designed and synthesized by click chemistry. All dimer analogues exhibited significantly improved antimicrobial activity against bacterial strains in vitro. The acute toxicity in mice of all dimer analogues was examined by us. All dimer analogues had potential therapeutic efficacy in a mouse bacteremia model infected by E. coli. All dimer analogues had membrane-active action mode and had α-helix conformation in 50% trifluoroethanol