Author/Authors :
Richard W. Friesen، نويسنده , , Daniel Dubé، نويسنده , , Rejean Fortin، نويسنده , , Richard Frenette، نويسنده , , Sylvie Prescott، نويسنده , , Wanda Cromlish، نويسنده , , Gillian M. Greig، نويسنده , , Stacia Kargman، نويسنده , , Elizabeth Wong، نويسنده , , Chi-Chung Chan، نويسنده , , Robert Gordon، نويسنده , , Li Jing Xu، نويسنده , , Denis Riendeau، نويسنده ,
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-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.
