Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors

The synthesis and activity of a series of 4,5-diarylimidazole analogs are described. One analog had an IC 50 of 80 nM, was 6750-selective against COX-1, and demonstrated in vivo potency in the mouse air pouch model. The synthesis and activity of a series of 4,5-diarylimidazole COX-2 inhibitors are d...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-12, Vol.8 (24), p.3443-3448
Hauptverfasser:	Barta, Thomas E., Stealey, Michael A., Collins, Paul W., Weier, Richard M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cyclooxygenase Inhibitors - pharmacology Imidazoles - chemistry Imidazoles - pharmacology Medical sciences Mice Molecular Structure Pharmacology. Drug treatments
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Beschreibung
Zusammenfassung:	The synthesis and activity of a series of 4,5-diarylimidazole analogs are described. One analog had an IC 50 of 80 nM, was 6750-selective against COX-1, and demonstrated in vivo potency in the mouse air pouch model. The synthesis and activity of a series of 4,5-diarylimidazole COX-2 inhibitors are described. One analog had an IC 50 of 80 nM, was 6750-fold selective against COX-1, and demonstrated in vivo potency in the mouse air pouch model.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00627-1