Synthesis and antimicrobial evaluation of cationic low molecular weight amphipathic 1,2,3-triazoles |
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| Authors: | Thomas A Bakka Morten B Strøm Jeanette H Andersen Odd R Gautun |
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| Institution: | 1. Department of Chemistry, Norwegian University of Science and Technology (NTNU), NO-7491 Trondheim, Norway;2. Department of Pharmacy, Faculty of Health Sciences, University of Tromsø, NO-9037 Tromsø, Norway;3. Marbio, Faculty of Biosciences, Fisheries and Economics, University of Tromsø, NO-9037 Tromsø, Norway |
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| Abstract: | 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 μg/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. |
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| Keywords: | Antibacterial Click chemistry Marine natural product mimics Peptidomimetics 1 2 3-Triazoles |
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