Shin Chung

2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors.

A new series of cyclooxygenase-2(COX-2) inhibitors with naturally occurring flavone as the main skeleton has been synthesized and their biological activities were evaluated for cyclooxygenase inhibitory activity. Rational structural modifications were applied to potent COX-2 inhibitors to obtain the desired pharmacokinetic profiles for improved oral anti-inflammatory activity.

2,2-Dimethyl-4,5-diaryl-3(2H)furanone derivatives as selective cyclo-oxygenase-2 inhibitors

A series of 2,2-dimethyl-5-[4-(methylsulfonyl)phenyl]-4-phenyl-3(2H)furanones was prepared and evaluated for their ability to inhibit cyclo-oxygenase-2 (COX-2).

Profiles of COX-2 inhibitors: present and future

Cyclooxygenases are responsible for the biosynthesis of prostanoids, the overt presence of which is often associated with inflammation and pain. Since the discovery of COX-2 in the last decade, a myriad of selective COX-2 inhibitors and their pharmacological profiles have been witnessed. Pharmacological observations of selective inhibition of COX-2 often go beyond initial expectations. This review is an overview of issues on selective COX-2 inhibitors, which include gastrointestinal and cardiovascular safety, emerging therapeutic areas and differentiation in drug profiles expected to be addressed by future generation COX-2 inhibitors. This article also covers recent patents and papers on new COX-2 inhibitors published since 2002. Future generation COX-2 inhibitors are sure to be safer and meet better medical needs than the COX-2 inhibitors currently available for the treatment or prevention of broadly ranged COX-2-mediated disorders.