Antiinflammatory 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones: Novel inhibitors of COX-2

A series of 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones was prepared. Members of this series are potent and selective inhibitors of cyclooxygenase-2 (COX-2) in both microsomal and cellular assays. Two representatives demonstrated activity in the carrageenan-induced paw edema model in rats upon or...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-05, Vol.8 (10), p.1181-1186
Main Authors: LAZER, E. S, SORCEK, R, CYWIN, C. L, THOME, D, POSSANZA, G. J, GRAHAM, A. G, CHURCHILL, L
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Carrageenan
Cyclooxygenase 1
Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors - chemical synthesis
Cyclooxygenase Inhibitors - chemistry
Cyclooxygenase Inhibitors - pharmacology
Edema - chemically induced
Edema - drug therapy
Isoenzymes - metabolism
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Isoquinolines - pharmacology
Kinetics
Medical sciences
Membrane Proteins
Microsomes - enzymology
Molecular Structure
Pharmacology. Drug treatments
Prostaglandin-Endoperoxide Synthases - metabolism
Rats
Structure-Activity Relationship
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Summary:A series of 2-benzyl-4-sulfonyl-4H-isoquinoline-1,3-diones was prepared. Members of this series are potent and selective inhibitors of cyclooxygenase-2 (COX-2) in both microsomal and cellular assays. Two representatives demonstrated activity in the carrageenan-induced paw edema model in rats upon oral administration.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00184-X