NOVEL 1,2-DIARYLCYCLOBUTENES - SELECTIVE AND ORALLY-ACTIVE COX-2 INHIBITORS

Authors
FRIESEN RW DUBE D FORTIN R FRENETTE R PRESCOTT S CROMLISH W GREIG GM KARGMAN S WONG E CHAN CC GORDON R XU LJ RIENDEAU D
Citation
Rw. Friesen et al., NOVEL 1,2-DIARYLCYCLOBUTENES - SELECTIVE AND ORALLY-ACTIVE COX-2 INHIBITORS, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2677-2682
Citations number
28
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
22
Year of publication
1996
Pages
2677 - 2682
Database
ISI
SICI code
0960-894X(1996)6:22<2677:N1-SAO>2.0.ZU;2-H
Abstract
A series of novel 2,3-diaryl-2-cyclobuten-1-ones have been synthesized and have been evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-I and COX-2. 4,4-Dimethyl-2-phenyl-3- [4-(methylsulfonyl)phenyl]cyclobutenone 22 was found to be highly sele ctive for inhibition of COX-2 and was orally active (ED(50) = 2.4 mg/k g) in the rat paw edema model. Copyright (C) 1996 Elsevier Science Ltd