Synthesis and Cyclooxygenase (COX-1/COX-2) Inhibiting Property of 3,4-Diarylfuranones.

593-601A series of diarylfuranone including some 5-hydroxy derivatives and naphthofuranones have been synthesized as a unique class of COX-1/COX-2 inhibitors. In contrast to the earlier report of structurally similar rofecoxib, these compounds have been characterized as nonselective but highly potent COX inhibitors. Structure Activity Relationship study confirmed that methoxy and methyl sulfanyl moieties are essential for COX activity and replacement or removal of any of this group affect COX-2 potency drastically rather than COX-1 efficacy. Studies on in vitro, in vivo screens and pharmacokinetics are discussed

Synthesis and cyclooxygenase (COX-1/COX-2) inhibiting property of 3,4-diarylfuranones

593-601A series of diarylfuranone including some 5-hydroxy derivatives and naphthofuranones have been synthesized as a unique class of COX-1/COX-2 inhibitors. In contrast to the earlier report of structurally similar rofecoxib, these compounds have been characterized as nonselective but highly potent COX inhibitors. Structure Activity Relationship study confirmed that methoxy and methyl sulfanyl moieties are essential for COX activity and replacement or removal of any of this group affect COX-2 potency drastically rather than COX-1 efficacy. Studies on in vitro, in vivo screens and pharmacokinetics are discussed