Synthesis, Biological Evaluation of Some Arylsulfonyl, Carboxamide Derivatives of 3-Methyl-1H-pyrazol-5(4H)-one

Synthesis of pyrazolone, its derivatives is of particular interest in heterocyclic chemistry due to their pharmaceutical importance. In the present study arylsulfonyl (1a-f, 2a-f), carboxamide (3a-e) derivatives of 3-methyl-1H-pyrazol-5(4H)-one were synthesized. The reaction of pyrazolone with arylsulfonyl chlorides resulted in mono (1a-f), disubstituted (2a-f) arylsulfonyl derivatives of 3-methyl-1H-pyrazol-5(4H)-one. On the other h,, the pyrazolone on treatment with different isocyanates yielded respective carboxamides (3a-e). The synthesized compounds were screened for urease inhibition, antibacterial, antioxidant assays, exhibit promising urease inhibition. Compound 1e was observed to be most active urease inhibitor in the series with 91.9 % inhibition. However, the antioxidant, antibacterial activities of all the compounds were non-significant at non-toxic concentration.