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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-05, Vol.8 (10), p.1181-1186
Hauptverfasser:	LAZER, E. S, SORCEK, R, CYWIN, C. L, THOME, D, POSSANZA, G. J, GRAHAM, A. G, CHURCHILL, L
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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