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- Title
DESIGN, SYNTHESIS OF SCHIFF BASE CIPROFLOXACIN - VANILLIN DERIVATIVES AS POTENT BACTERIAL DNA GYRASE INHIBITORS.
- Authors
Sekhar, Swain Sudhansu; Ranjan, Sahoo Chita; Jyotirmaya, Sahoo; Nath, Padhy Rabindra; B. V. V., Ravi Kumar; Kumar, Paidesetty Sudhir
- Abstract
A series of Schiff base ciprofloxacin hydrazones with vanillin analogues were designed and validated for druggability properties by advanced computational tools, from which two shortlisted compounds were synthesized and characterized by different spectral studies. These compounds were used against bacterial DNA gyrase; purposedly attempted in molecular docking studies, the compounds 5h and 5i indicated good binding affinity of -8.2 and -8.5 kcal/mol, respectively. Moreover, in vitro antibacterial activities against uropathogenic bacteria, E. coli, was assessed and the compounds 5h, and 5i had significant inhibitory actions. SAR studies revealed that the presence of the quinolone nucleus, azomethine functional group and vanillyl ester might have shown the response of antibacterial inhibition. Thus, vanillyl esters condensed with ciprofloxacin hydrazone through Schiff base, have more antibacterial inhibitory actions. The recorded antibacterial results were corroborated with docking results.
- Subjects
DNA topoisomerase II; BACTERIAL DNA; SCHIFF bases; VANILLIN; CIPROFLOXACIN; ESTERS; DNA synthesis
- Publication
Indian Drugs, 2020, Vol 57, Issue 3, p21
- ISSN
0019-462X
- Publication type
Article
- DOI
10.53879/id.57.03.12279