Université Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, 63000, Clermont-Ferrand, France.
Université Clermont Auvergne, CNRS, LMGE, 63000, Clermont-Ferrand, France.
ChemMedChem. 2018 Aug 10;13(15):1513-1516. doi: 10.1002/cmdc.201800273. Epub 2018 Jul 4.
Amphipathic cationic peptoids (N-substituted glycine oligomers) represent a promising class of antimicrobial peptide mimics. The aim of this study is to explore the potential of the triazolium group as a cationic moiety and helix inducer to develop potent antimicrobial helical peptoids. Herein we report the first solid-phase synthesis of peptoid oligomers incorporating 1,2,3-triazolium-type side chains and their evaluation against Escherichia coli, Enterococcus faecalis, and Staphylococcus aureus. Several triazolium-based oligomers, even of short length, selectively kill bacteria over mammalian cells. SEM visualization of S. aureus cells treated with a dodecamer and a hexamer reveals severe cell membrane damage and suggests that the longer oligomer acts by pore formation.
两亲性阳离子缩氨酸（N-取代甘氨酸寡聚物）是一类很有前途的抗菌肽模拟物。本研究旨在探索三唑基团作为阳离子部分和螺旋诱导物的潜力，以开发有效的抗菌螺旋缩氨酸。本文首次报道了在固相合成中引入 1,2,3-三唑型侧链的缩氨酸寡聚物及其对大肠杆菌、粪肠球菌和金黄色葡萄球菌的评价。几种三唑基寡聚物，即使长度较短，也能选择性地杀死细菌而不杀伤哺乳动物细胞。用十二聚体和六聚体处理金黄色葡萄球菌细胞的 SEM 可视化显示出严重的细胞膜损伤，并表明较长的寡聚物通过形成孔起作用。
