SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL PYRAZOLINE DERIVATIVES DERIVED FROM N-SUBSTITUTED QUINOLINYL CHALCONES

A series of novel substituted 1-amino-3-(5-phenyl-4, 5-dihydro-1H-pyrazol-3-yl) quinolin-2(1H)-one (AJP1-AJP8) have been synthesized upon reaction with 1-amino-3-cinnamoyl-quinolin-2(1H)-one by using hydrazine hydrate as cyclising medium in alcohol medium. 1-amino-3-cinnamoyl-quinolin-2(1H)-one were synthesized by condensing 3-acetyl-1-amino-quinolin-2-one with different substituted benzaldehyde in presence of ethanolic KOH. The structures of the final synthesized compounds were confirmed by IR, 1H NMR and mass spectra. The synthesized compounds were screened for their antibacterial and antifungal activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans, Aspergillus niger respectively by cup plate method. Compounds AJP1, AJP3, AJP4, AJP5, AJP6 and AJP7 showed good antibacterial activity compared to the standard drug amoxicillin. Compounds AJP1, AJP3, AJP5 and AJP7 showed moderate antifungal activity compared to the standard drug fluconazole. The synthesized compounds were screened for their anti-inflammatory activity by Carrageenan induced paw edema method. Compounds AJP1 and AJP7 showed significant anti-inflammatory activity compared to the standard drug diclofenac sodium