Bioorganic & medicinal chemistry letters, 2017-03, Vol.27 (5), p.1119-1123
2017
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and antimicrobial evaluation of cationic low molecular weight amphipathic 1,2,3-triazoles
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2017-03, Vol.27 (5), p.1119-1123
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2017
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- [Display omitted] 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 4–8μg/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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2017.01.092Titel-ID: cdi_proquest_miscellaneous_1867983168
- Format
- –
- Schlagworte
- 1,2,3-Triazoles, Anti-Bacterial Agents - chemical synthesis, Anti-Bacterial Agents - chemistry, Anti-Bacterial Agents - pharmacology, Antibacterial, Cations, Click chemistry, Gram-Negative Bacteria - drug effects, Gram-Positive Bacteria - drug effects, Marine natural product mimics, Microbial Sensitivity Tests, Molecular Weight, Peptidomimetics, Triazoles - chemical synthesis, Triazoles - chemistry, Triazoles - pharmacology