Antibacterial and Urease Inhibitory activity of New Piperazinyl N-4 Functionalized Ciprofloxacin-oxadiazoles | ||
| Journal of Modern Research | ||
| Article 1, Volume 1, Issue 1, July 2019, Pages 1-7 PDF (1.27 M) | ||
| Document Type: Research Articles | ||
| DOI: 10.21608/jmr.2019.12650.1001 | ||
| Authors | ||
| Mohamed A.A. Abdel-Aal1; Salah A. Abdel-Aziz1; Montaser Sh. A. Shaykoon1; Mamdouh F. A. Mohamed2; Gamal El-Din A.A. Abuo-Rahma* 3 | ||
| 1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt | ||
| 2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sohag University, Sohag 82524, Egypt | ||
| 3Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt | ||
| Abstract | ||
| This research includes design of new ciprofloxacin bearing oxadiazole at the N-4 piperazinyl for the purpose of having urease inhibitory activity as well as antibacterial activity. Hence, a group of new N-4 piperazinyl oxdiazole derivatives of ciprofloxacin was prepared and characterized using different spectroscopic and analytical techniques including 1H-NMR, 13C-NMR, MS and elemental analysis. Compounds 5b and 5c experienced moderate activity against the urease producing Klebsiella pneumoniae strains better than the standard drug used chloramphenicol and less than the parent drug ciprofloxacin. On the other hand, most of the tested compounds showed a urease inhibitory activity more than the parent drug, ciprofloxacin and comparable to standard, thiourea. The docked compounds exhibited better binding to urease enzyme of H. pylori than standard, AHA with binding scores for correlate to the anti-urease assay results. Compound 5b was the most potent anti-Klebsiella pneumoniae urease inhibitor with activity higher the standard (IC50 = 67.8 and 78.89 µM, respectively). | ||
| Keywords | ||
| ciprofloxacin; Oxadiazole; Antibacterial; Urease inhibitors; Molecular docking | ||
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