Volume 28, Issue 36
Heterocyclic Compounds
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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).

T. D. PENNING

T. D. PENNING

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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J. J. TALLAY

J. J. TALLAY

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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S. R. BERTENSHAW

S. R. BERTENSHAW

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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J. S. CARTER

J. S. CARTER

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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P. W. COLLINS

P. W. COLLINS

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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S. DOCTER

S. DOCTER

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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M. J. GRANETO

M. J. GRANETO

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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L. F. LEE

L. F. LEE

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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J. W. MALECHA

J. W. MALECHA

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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J. M. MIYASHIRO

J. M. MIYASHIRO

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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ET AL. ET AL.

ET AL. ET AL.

Dep. Chem., G. D. Searle Co., Skokie, IL 60077, USA

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First published: 03 August 2010
Citations: 20

Abstract

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ChemInform Abstract

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.

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