Synthesis and antimicrobial evaluation of cationic low molecular weight amphipathic 1,2,3-triazoles

被引：13

作者：

Bakka, Thomas A. ^{[1
]}

Strom, Morten B. ^{[2
]}

Andersen, Jeanette H. ^{[3
]}

Gautun, Odd R. ^{[1
]}

机构：

[1] Norwegian Univ Sci & Technol NTNU, Dept Chem, NO-7491 Trondheim, Norway

[2] Univ Tromso, Fac Hlth Sci, Dept Pharm, NO-9037 Tromso, Norway

[3] Univ Tromso, Fac Biosci Fisheries & Econ, Marbio, NO-9037 Tromso, Norway

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 05期

关键词：

Antibacterial; Click chemistry; Marine natural product mimics; Peptidomimetics; 1,2,3-Triazoles; 1,3-DIPOLAR CYCLOADDITION; ANTIBACTERIAL PEPTIDES; AZIDES; RESISTANCE; BACTERIA; ALKYNES; AMINES; HYDROCHLORIDE; ANTIBIOTICS; ROTAXANES;

D O I：

10.1016/j.bmcl.2017.01.092

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A library of 28 small cationic 1,4-substituted 1,2,3-triazoles was prepared for studies of antimicrobial activity. The structures addressed the pharmacophore model of small antimicrobial peptides and an amphipathic motif found in marine antimicrobials. Eight compounds showed promising antimicrobial activity, of which the most potent compound 10b displayed minimum inhibitory concentrations of 4-8 mu g/mL against Streptococcus agalacticae, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Enterococcus faecalis. The simple syntheses and low degree of functionalization make these 1,4-substituted 1,2,3-triazoles interesting for further optimizations. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：1119 / 1123

页数：5

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