Synthesis and antimicrobial activity of some new pyrazole containing cyanopyridone derivatives
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Date
2012
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Abstract
A series of new 4,6-disubstituted-3-cyano-2-pyridone derivatives (4a-o) were synthesized. The structures of all target molecules (4a-o) have been confirmed by various spectral techniques and elemental analyses. The newly synthesized compounds were screened for antibacterial and antifungal activity and most of the compounds showed significant activity comparable with that of the standard drug. The results revealed that 4b, 4c, 4d, 4g, 4m, 4n and 4o showed good antibacterial activity towards all bacterial strains (Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa) when compared to standard drug streptomycin. Amongst all the compounds, 4c showed moderate antifungal activity against Aspergillus flavus. The acute toxicity study has also been carried out for biologically active compounds and the experimental studies revealed that compounds were safe up to 2000 mg/kg and no deaths of animals were recorded.
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2 oxo 4 (3 phenyl 1h pyrazol 4 yl) 6 (thiophen 2 yl) 1,2 dihydropyridine 3 carbonitrile, 4 [3 (2,4 dichlorophenyl) 1h pyrazol 4 yl] 6 (naphthalen 1 yl) 2 oxo 1,2 dihydropyridine 3 carbonitrile, 4 [3 (2,4 dichlorophenyl)1h pyrazol 4 yl] 2 oxo 6 (thiophen 2 yl) 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 chlorophenyl) 1h pyrazol 4 yl] 6 (5 chlorothiopen 2 yl) 2 oxo 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 chlorophenyl) 1h pyrazol 4 yl] 6 (naphthalen 1 yl) 2 oxo 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 chlorophenyl)1h pyrazol 4 yl] 2 oxo 6 (thiophen 2 yl) 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 fluorophenyl) 1h pyrazol 4 yl] 6 (naphthalen 1 yl) 2 oxo 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 fluorophenyl)1h pyrazol 4 yl] 2 oxo 6 (thiophen 2 yl) 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 methoxyphenyl) 1h pyrazol 4 yl] 6 (naphthalen 1 yl) 2 oxo 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 methylphenyl) 1h pyrazol 4 yl] 6 (naphthalen 1 yl) 2 oxo 1,2 dihydropyridine 3 carbonitrile, 4 [3 (4 methylphenyl)1h pyrazol 4 yl] 2 oxo 6 (thiophen 2 yl) 1,2 dihydropyridine 3 carbonitrile, 4,6 disubstituted 3 cyano 2 pyridone derivative, 6 (5 chlorothiophen 2 yl) 2 oxo 4 (3 phenyl 1h pyrazol yl) 1,2 dihydropyridine 3 carbonitrile, 6 (5 chlorothiophen 2 yl) 4 [3 (4 fluorophenyl) 1h pyrazol 4 yl] 2 oxo 1,2 dihydropyridine 3 carbonitrile, 6 (5 chlorothiophen 2 yl) 4 [3 (4 methylphenyl) 1h pyrazol 4 yl] 2 oxo 1,2 dihydropyridine 3 carbonitrile, 6 (naphthalen 1 yl) 2 oxo 4 (3 phenyl 1h pyrazole 4 yl) 1,2 dihydropyridine 3 carbonitrile, pyrazole derivative, unclassified drug, animal experiment, animal model, antibacterial activity, antifungal activity, article, Aspergillus flavus, bacterial strain, controlled study, drug efficacy, drug safety, drug structure, drug synthesis, Escherichia coli, fungal strain, male, nonhuman, Pseudomonas aeruginosa, rat, Staphylococcus aureus, toxicity testing
Citation
Der Pharma Chemica, 2012, 4, 1, pp. 43-52