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

• DOI: 10.1016/j.ejmech.2017.10.042
• Publication Date: 2017-10-16T16:32:31Z
• Authors: Hassan M. Faidallah; Adel S. Girgis; Anand D. Tiwari; Hitesh H. Honkana...; Sean J. Thomas; Ahmed Samir; Atef Kalmouch; Khalid A. Alamry; Khalid A. Khan; Tarek S. Ibrahim; Amany M.M. AL-Mah...; Abdullah M. Asiri; Siva S. Panda
• Keywords: Conjugate; Quinolone; Bacteria; QSAR; 1,2,3-Triazole; Quantitative Structure-Activity Relationship; Chemistry Techniques, Synthetic; Microbial Sensitivity Tests; Quinolones; Triazoles; 01 natural sciences; Anti-Bacterial Agents; 0104 chemical sciences; Antibacterial

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.