کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1375962 | 981947 | 2009 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide](/preview/png/1375962.png)
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 (3k–m) showed COX-1 and COX-2 inhibitory activity at 0.05 μM.
We prepared 19 new pyrazoline derivatives and evaluated for their anti-inflammatory potential in rats and also in vitro COX-1 and COX-2 enzyme inhibition using recombinant enzymes. Four compounds were found to be more active than celecoxib, a clinically used anti-inflammatory drug and they also inhibited COX-1 and COX-2.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 1, 1 January 2009, Pages 255–258