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Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide.

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, (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 60 mg/kg. Compounds (3k-m) showed COX-1 and COX-2 inhibitory activity at 0.05 microM.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Rathish IG,Javed K,Ahmad S,Bano S,Alam MS,Pillai KK,Singh S,Bagchi V

doi

10.1016/j.bmcl.2008.10.105

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

255-8

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01294-8

journal_volume

19

pub_type

杂志文章

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