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...

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Veröffentlicht in:European journal of medicinal chemistry 2018-01, Vol.143, p.1524-1534
Hauptverfasser: Faidallah, Hassan M., Girgis, Adel S., Tiwari, Anand D., Honkanadavar, Hitesh H., Thomas, Sean J., Samir, Ahmed, Kalmouch, Atef, Alamry, Khalid A., Khan, Khalid A., Ibrahim, Tarek S., AL-Mahmoudy, Amany M.M., Asiri, Abdullah M., Panda, Siva S.
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Sprache:eng
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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