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Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide
Authors:I.G. Rathish  Kalim Javed  Shamim Ahmad  Sameena Bano  M.S. Alam  K.K. Pillai  Surender Singh  Vivek Bagchi
Affiliation:1. Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110 062, India;2. Department of Pharmacology, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi 110 062, India;3. Department of Pharmacology, All India Institute of Medical Sciences, New Delhi 110 029, India;4. Department of Chemistry, Indian Institute of Technology, New Delhi 110 016, India
Abstract: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, 1H NMR, 13C NMR, mass spectroscopic and elemental analyses data. These compounds were tested at dose of 20 mg/kg for their anti-inflammatory activity in carrageenan-induced rat paw edema model and volume of paw edema was measured at 0, 3 and 5 h. Two compounds 3k and 3l were found to be more active than celecoxib throughout the study (at 3 and 5 h). While two other compounds 3m and 3n showed more potent activity than celecoxib at 5 h. They are devoid of ulcerogenic potential when administered orally at a dose of 60 mg/kg. Compounds (3km) showed COX-1 and COX-2 inhibitory activity at 0.05 μM.
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