ChemInform Abstract: Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors: Identification of 4-(5-(4-Methylphenyl)-3- (trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide (SC-58635, Celecoxib).
β Scribed by T. D. PENNING; J. J. TALLAY; S. R. BERTENSHAW; J. S. CARTER; P. W. COLLINS; S. DOCTER; M. J. GRANETO; L. F. LEE; J. W. MALECHA; J. M. MIYASHIRO; ET AL. ET AL.
- Publisher
- John Wiley and Sons
- Year
- 2010
- Weight
- 35 KB
- Volume
- 28
- Category
- Article
- ISSN
- 0931-7597
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β¦ Synopsis
Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors: Identification of 4-(5-(4-Methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide (SC-58635, Celecoxib).
-Claisen condensation, followed by regioselective reaction with the hydrochloride of arylhydrazines yields almost exclusively 1,5-diarylpyrazoles. Among a series of derivatives, e.g. (I), (II), and ( III), only title compound (Ib) is of interest for further evaluation in clinical trials concerning treatment of rheumatoid arthritis and osteoarthritis. -(PENNING, T. D.;
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## Abstract The results of biological tests show that compound (I) is a potent and selective inhibitor of COXβ2 (IC~50~ = 0.37 ΞΌM) being equipotent to celecoxib.
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