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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
- 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.
- Subjects :
- Quantitative structure–activity relationship
biology
Stereochemistry
Aryl
General Medicine
medicine.disease_cause
biology.organism_classification
Ciprofloxacin
chemistry.chemical_compound
chemistry
Staphylococcus aureus
Carboxylic acid synthesis
medicine
Tetrazole
Antibacterial activity
Bacteria
medicine.drug
Subjects
Details
- ISSN :
- 09317597
- Volume :
- 45
- Database :
- OpenAIRE
- Journal :
- ChemInform
- Accession number :
- edsair.doi...........aaff410ef679853a3794b556f6624bfd