当前位置: X-MOL 学术ChemMedChem › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
1,2,3‐Triazolium‐Based Cationic Amphipathic Peptoid Oligomers Mimicking Antimicrobial Helical Peptides
ChemMedChem ( IF 3.4 ) Pub Date : 2018-07-04 , DOI: 10.1002/cmdc.201800273
Radhe Shyam 1 , Nicolas Charbonnel 2 , Aurélie Job 1 , Christelle Blavignac 3 , Christiane Forestier 2 , Claude Taillefumier 1 , Sophie Faure 1
Affiliation  

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.

中文翻译:

基于1,2,3-三唑鎓的模仿抗菌螺旋肽的阳离子两亲拟肽寡聚体

两亲性阳离子类肽(N取代的甘氨酸低聚物)代表了有希望的一类抗菌肽模拟物。这项研究的目的是探索三唑鎓基团作为阳离子部分和螺旋诱导剂开发有效的抗菌螺旋类肽的潜力。本文中我们报道了结合1,2,3-三唑类侧链的类肽低聚物的第一个固相合成及其对大肠杆菌粪肠球菌金黄色葡萄球菌的评价。几种基于三唑鎓的低聚物,即使长度很短,也可以选择性杀死哺乳动物细胞上的细菌。金黄色葡萄球菌的SEM可视化 用十二聚体和六聚体处理的细胞显示出严重的细胞膜损伤,并表明较长的低聚物通过孔形成起作用。
更新日期:2018-07-04
down
wechat
bug