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 Shankar Panda

Research output: Contribution to journalArticle

11 Citations (Scopus)

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

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Triazoles
Quantitative Structure-Activity Relationship
Quinolones
Click Chemistry
Anti-Bacterial Agents
Microwaves
Gram-Negative Bacteria
Bacteria

Keywords

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

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

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

In: European Journal of Medicinal Chemistry, Vol. 143, 01.01.2018, p. 1524-1534.

Research output: Contribution to journalArticle

Faidallah, HM, Girgis, AS, Tiwari, AD, Honkanadavar, HH, Thomas, SJ, Samir, A, Kalmouch, A, Alamry, KA, Khan, KA, Ibrahim, TS, AL-Mahmoudy, AMM, Asiri, AM & Panda, SS 2018, 'Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates', European Journal of Medicinal Chemistry, vol. 143, pp. 1524-1534. https://doi.org/10.1016/j.ejmech.2017.10.042
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 Shankar. / Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates. In: European Journal of Medicinal Chemistry. 2018 ; Vol. 143. pp. 1524-1534.
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