title: Synthesis of pyrazole encompassing 2-pyridone derivatives as antibacterial agents.
abstract: A series of novel compounds 6-amino-1-((1,3-diphenyl-1H-pyrazole-4-yl)methyleneamino)-4-(aryl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitriles (4a-t) were synthesized and characterized by IR, (1)H NMR, (13)C NMR and mass spectral data. These compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, Streptococcus pyogenes (Gram positive), Escherichia coli, Pseudomonas aeruginosa (Gram negative) by serial broth dilution and cytotoxic activity (NIH 3T3 & HeLa) by MTT assay. The results indicated that compounds 4g, 4i, 4m, 4o, 4r and 4t exhibit potent antibacterial activity against bacterial strains at non-cytotoxic concentrations.
authors.affiliation: Division of Medicinal Chemistry, Department of Chemistry, (DST-FIST Sponsored Department) Mahatma Gandhi Campus, Maharaja Krishnakumarsinhji Bhavnagar University, Bhavnagar 364 002, India. dnisheeth@rediffmail.com
authors.forename: Nisheeth C
authors.initials: NC
authors.lastname: Desai
authors.forename: Kiran M
authors.initials: KM
authors.lastname: Rajpara
authors.forename: Vivek V
authors.initials: VV
authors.lastname: Joshi
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D008826:Microbial Sensitivity Tests; D041681:NIH 3T3 Cells; D011720:Pyrazoles / Q000737:chemistry*; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D011720:Pyrazoles; D011728:Pyridones; C031280:pyrazole; C017679:2-hydroxypyridine