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Design of Triazolium-Grafted Peptidomimetic Macrocycles with Facial Amphipathicity to Target Pathogenic Bacteria
Organic Letters ( IF 5.2 ) Pub Date : 2024-05-06 , DOI: 10.1021/acs.orglett.4c01149
Cassandra Guerinot 1 , Mélodie Malige 2 , Nicolas Charbonnel 2 , Killian Malosse 1 , Laurent Jouffret 1 , Claude Taillefumier 1 , Olivier Roy 1 , Christiane Forestier 2 , Sophie Faure 1
Affiliation  

Access to 1,2,3-triazolium-grafted peptoid macrocycles was developed by macrocyclization and multivalent postmodification of linear peptoid oligomers carrying an alternance of benzylic and propargyl groups as side chains. X-ray analysis and NMR studies revealed a conformational preference for constrained hairpin-shaped structures leading to the facial amphipathic character of these macrocycles. A preliminary evaluation showed the antimicrobial activities of these new cationic amphipathic architectures.

中文翻译:

具有表面两亲性的三唑接枝拟肽大环化合物针对病原菌的设计

通过对带有交替的苄基和炔丙基基团作为侧链的线性类肽寡聚物进行大环化和多价后修饰,开发了 1,​​2,3-三唑鎓接枝的类肽大环化合物。 X 射线分析和核磁共振研究揭示了对受限发夹形结构的构象偏好,导致这些大环化合物的表面两亲性特征。初步评估显示了这些新型阳离子两亲结构的抗菌活性。
更新日期:2024-05-06
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