Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors

A series of novel sulfone substituted 4,5-diarylthiazoles have been synthesized and evaluated for their inhibition of the two isoforms of human cyclooxygenase (COX-1 and COX-2). This series displays exceptionally selective COX-2 inhibition. A series of novel sulfone substituted 4,5-diarylthiazoles w...

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Published inBioorganic & medicinal chemistry letters Vol. 9; no. 8; pp. 1167 - 1170
Main Authors Carter, Jeffery S., Rogier, D.J., Graneto, Matthew J., Seibert, Karen, Koboldt, Carol M., Yan Zhang, Talley, John J.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 19.04.1999
Elsevier
Subjects
Animals
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cyclooxygenase 2
Inhibitory Concentration 50
Isoenzymes - drug effects
Medical sciences
Pharmacology. Drug treatments
Prostaglandin-Endoperoxide Synthases - drug effects
Rats
Sulfones - chemistry
Thiazoles - chemical synthesis
Human
Sulfur nitrogen heterocycle
Prostaglandin-endoperoxide synthase
Sulfone
Enzyme
Isozyme
Thiazole derivatives
Benzene derivatives
Enzyme inhibitor
Selectivity
In vitro
Structure activity relation
Chlorine Organic compounds
Fluorine Organic compounds
Oxidoreductases
Chemical synthesis
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Summary:A series of novel sulfone substituted 4,5-diarylthiazoles have been synthesized and evaluated for their inhibition of the two isoforms of human cyclooxygenase (COX-1 and COX-2). This series displays exceptionally selective COX-2 inhibition. A series of novel sulfone substituted 4,5-diarylthiazoles were synthesized and shown to display exceptionally selective COX-2 inhibition.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00158-4