Novel 1, 2-diarylcyclobutenes: Selective and orally active COX-2 inhibitors

…, R Fortin, R Frenette, S Prescott, W Cromlish…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 22 p. 2677 - 2682

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Citation Number: 41

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.