Small molecule mimics of DFTamP1, a database designed anti-Staphylococcal peptide

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• 作者：Yuxiang Dong^a ; ^{ydong@unmc.edu} ; Tamara Lushnikova^b ; Radha M. Golla^b ; Xiaofang Wang^a ; Guangshun Wang^b ; ^{gwang@unmc.edu}
• 关键词：Antimicrobial peptides ; Chemical synthesis ; Database filtering technology ; Peptide mimics
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：864-869
• 全文大小：1014 K
• 卷排序：25

文摘

Antimicrobial peptides (AMPs) are important templates for developing new antimicrobial agents. Previously, we developed a database filtering technology that enabled us to design a potent anti-Staphylococcal peptide DFTamP1. Using this same design approach, we now report the discovery of a new class of bis-indole diimidazolines as AMP small molecule mimics. The best compound killed multiple S. aureus clinical strains in both planktonic and biofilm forms. The compound appeared to target bacterial membranes with antimicrobial activity and membrane permeation ability similar to daptomycin.