Design, synthesis, molecular docking, and antibacterial evaluation of some novel flouroquinolone derivatives as potent antibacterial agent.

Autor: Patel MM; Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, CHARUSAT Campus, Changa, Petlad Taluka, Anand District, Gujarat 388 421, India., Patel LJ; S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Kherva, Gujarat 382711, India.
Jazyk: angličtina
Zdroj: TheScientificWorldJournal [ScientificWorldJournal] 2014; Vol. 2014, pp. 897187. Date of Electronic Publication: 2014 Dec 09.
DOI: 10.1155/2014/897187
Abstrakt: Objective: Quinolone moiety is an important class of nitrogen containing heterocycles widely used as key building blocks for medicinal agents. It exhibits a wide spectrum of pharmacophores and has bactericidal, antiviral, antimalarial, and anticancer activities. In view of the reported antimicrobial activity of various fluoroquinolones, the importance of the C-7 substituents is that they exhibit potent antimicrobial activities. Our objective was to synthesize newer quinolone analogues with increasing bulk at C-7 position of the main 6-fluoroquinolone scaffold to produce the target compounds which have potent antimicrobial activity.
Methods: A novel series of 1-ethyl-6-fluoro-4-oxo-7-{4-[2-(4-substituted phenyl)-2-(substituted)-ethyl]-1-piperazinyl}-1,4-dihydroquinoline-3-carboxylic acid derivatives were synthesized. To understand the interaction of binding sites with bacterial protein receptor, the docking study was performed using topoisomerase II DNA gyrase enzymes (PDB ID: 2XCT) by Schrodinger's Maestro program. In vitro antibacterial activity of the synthesized compounds was studied and the MIC value was calculated by the broth dilution method.
Results: Among all the synthesized compounds, some compounds showed potent antimicrobial activity. The compound 8g exhibited good antibacterial activity.
Conclusion: This investigation identified the potent antibacterial agents against certain infections.
Databáze: MEDLINE
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