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Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates

Authors :
Khalid A. Khan
Amany M.M. Al-Mahmoudy
Abdullah M. Asiri
Hassan M. Faidallah
Ahmed Samir
Khalid A. Alamry
Tarek S. Ibrahim
Sean J. Thomas
Siva S. Panda
Hitesh H. Honkanadavar
Adel S. Girgis
Anand D. Tiwari
Atef Kalmouch
Source :
European Journal of Medicinal Chemistry. 143:1524-1534
Publication Year :
2018
Publisher :
Elsevier BV, 2018.

Abstract

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.

Details

ISSN :
02235234
Volume :
143
Database :
OpenAIRE
Journal :
European Journal of Medicinal Chemistry
Accession number :
edsair.doi.dedup.....49e0ecc501011eaf2b40e747271cf469
Full Text :
https://doi.org/10.1016/j.ejmech.2017.10.042