Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide. Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] Journal article

Nineteen new 2-pyrazoline bearing benzenesulfonamide derivatives were synthesized by condensing chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride. Their chemical structures were proved by means of IR, (1)H NMR, (13)C NMR, mass spectroscopic and elemental analyses data. These compounds were tested at dose of 20mg/kg for their anti-inflammatory activity in carrageenan-induced rat paw edema model and volume of paw edema was measured at 0, 3 and 5h. Two compounds 3k and 3l were found to be more active than celecoxib throughout the study (at 3 and 5h). While two other compounds 3m and 3n showed more potent activity than celecoxib at 5h. They are devoid of ulcerogenic potential when administered orally at a dose of 60mg/kg. Compounds (3k-m) showed COX-1 and COX-2 inhibitory activity at 0.05muM.

Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett]