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ChemInform Abstract: Investigation of Ugi-4CC Derived 1H-Tetrazol-5-yl-(aryl) Methyl Piperazinyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid: Synthesis, Biology and 3D-QSAR Analysis

Authors :
Pratiksha Singh
Vikash Kumar
Praveen K. Shukla
Mohammad Imran Siddiqi
Kuldeep Chauhan
Prem M. S. Chauhan
Source :
ChemInform. 45
Publication Year :
2014
Publisher :
Wiley, 2014.

Abstract

Novel series of 7-piperazinylquinolones with tetrazole derivatives were synthesized and evaluated for their antibacterial activity against various strains of Staphylococcus aureus. All the synthesized compounds showed significant in vitro antibacterial activity against Gram-positive bacteria whereas some compounds displayed moderate activity against Gram-negative bacteria. Among all the synthesized compounds, compounds (6a-c, 6e-g, 6i-k, 6m, 6'f and 6'm) were found to be more effective with MIC ranging from (0.78-3.12 μg/mL) against S. aureus (ATCC-29213) than the control; ciprofloxacin (MIC = 25 μg/mL). Moreover, these analogues displayed no toxicity up to MIC = 0.39 μg/mL against mammalian cell line L-929. Furthermore, to correlate the biological activities of synthesized compounds with their 3D conformation, we attempted 3D-QSAR study.

Details

ISSN :
09317597
Volume :
45
Database :
OpenAIRE
Journal :
ChemInform
Accession number :
edsair.doi...........aaff410ef679853a3794b556f6624bfd