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

  • Eur J Med Chem. 2018 Jan 1;143:1524-1534. doi: 10.1016/j.ejmech.2017.10.042.
Hassan M Faidallah  1 ,  Adel S Girgis  2 ,  Anand D Tiwari  3 ,  Hitesh H Honkanadavar  4 ,  Sean J Thomas  4 ,  Ahmed Samir  5 ,  Atef Kalmouch  6 ,  Khalid A Alamry  1 ,  Khalid A Khan  1 ,  Tarek S Ibrahim  7 ,  Amany M M Al-Mahmoudy  8 ,  Abdullah M Asiri  1 ,  Siva S Panda  9
Affiliations
  • 1. Department of Chemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
  • 2. Pesticide Chemistry Department, National Research Centre, Dokki, Giza 12622, Egypt.
  • 3. Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA.
  • 4. Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA.
  • 5. Microbiology Department, Faculty of Veterinary Medicine, Cairo University, Cairo, Egypt.
  • 6. Peptide Chemistry Department, National Research Centre, Dokki, Giza 12622, Egypt.
  • 7. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Egypt.
  • 8. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Egypt.
  • 9. Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA. Electronic address: [email protected].
PMID: 29126731 DOI: 10.1016/j.ejmech.2017.10.042
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.

Keywords
1,2,3-Triazole; Antibacterial; Conjugate; QSAR; Quinolone.
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