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

Hassan M. Faidallah, Adel S. Girgis, Anand D. Tiwari, Hitesh H. Honkanadavar, Sean J. Thomas, Ahmed Samir, Atef Kalmouch, Khalid A. Alamry, Khalid A. Khan, Tarek S. Ibrahim, Amany M.M. AL-Mahmoudy, Abdullah M. Asiri, Siva S. Panda

Research output: Contribution to journalArticle

20 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)1524-1534
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume143
DOIs
StatePublished - Jan 1 2018

Keywords

  • 1,2,3-Triazole
  • Antibacterial
  • Conjugate
  • QSAR
  • Quinolone

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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  • Cite this

    Faidallah, H. M., Girgis, A. S., Tiwari, A. D., Honkanadavar, H. H., Thomas, S. J., Samir, A., Kalmouch, A., Alamry, K. A., Khan, K. A., Ibrahim, T. S., AL-Mahmoudy, A. M. M., Asiri, A. M., & Panda, S. S. (2018). Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates. European Journal of Medicinal Chemistry, 143, 1524-1534. https://doi.org/10.1016/j.ejmech.2017.10.042