Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates
A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10–15, 17–19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17–19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and...
Gespeichert in:
Veröffentlicht in: | European journal of medicinal chemistry 2018-01, Vol.143, p.1524-1534 |
---|---|
Hauptverfasser: | , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10–15, 17–19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17–19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1–3. 2D-QSAR modeling supports the observed biological properties.
[Display omitted]
•Quinolone-triazole conjugates were synthesized.•Some of the synthesized conjugates revealed promising antibacterial properties.•Statistically significant 2D-QSAR models support the biological properties. |
---|---|
ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2017.10.042 |