A series of novel fluorine containing pyrazole-pyrazolone (4a–j) and chromone-pyrazolone (5a–i) was synthesized from multifluorinated pyrazolone by the Knoevenagel condensation reaction. All compounds were synthesized by conventional heating as well as ultrasound irradiation technique. It was found that ultrasonication method was more efficient than conventional heating method. The newly synthesized compounds were subjected forin vitroantimicrobial screening against four bacterial pathogens, namely,Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli,andPseudomonas aeruginosaand three fungal pathogensCandida albicans, Aspergillus niger,andAspergillus clavatus, using broth microdilution (MIC) method (CLSI guidelines). Among them, some compounds exhibited promising antibacterial activity against the tested strains. All synthesized compounds were characterized by IR,1H-NMR, mass, and elemental analysis.
In present work the 4-formyl pyrazole (1) were treated with 4-morpholinoacetophene (2) in the presence of aqueous KOH to give Chalcones (3). The chalcones are subjected to react with malononitrile using sodium methoxide as a base in methanol to give pyridine-3-carbonitriles (4). The synthesized chalcone and pyridine-3-carbonitrile derivatives were subjected for study of their antiinflammatory activity by the well known carrageenan induced rat paw edema method. The products 3a, 3e and 4e exhibited good activity as compared with standard diclofenac drug. The formation of all compounds was established by the spectral techniques such as Infra Red, 1 H-NMR and mass.
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