Bioorganic and Medicinal Chemistry Letters p. 2677 - 2682 (1996)
Update date:2022-08-02
Topics:
Friesen, Richard W.
Dube, Daniel
Fortin, Rejean
Frenette, Richard
Prescott, Sylvie
Cromlish, Wanda
Greig, Gillian M.
Kargman, Stacia
Wong, Elizabeth
Chan, Chi Chung
Gordon, Robert
Xu, Li Jing
Riendeau, Denis
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-1 and COX-2. 4,4-Dimethyl-2-phenyl-3-[4-(methylsulfonyl)phenyl]cyclobutenone 22 was found to be highly selective for inhibition of COX-2 and was orally active (ED50 = 2.4 mg/kg) in the rat paw edema model.
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