Stephen R. Bertenshaw

Conformationally restricted 1,5-diarylpyrazoles are selective COX-2 inhibitors

Abstract Benzothiopyranopyrazoles and benzopyranopyrazoles containing either a sulfone or sulfonamide moiety were synthesized and tested for COX-1 and COX-2 inhibition. This new class of COX-2 selective inhibitors possess antiinflammatory activity in vivo.

3,4-diarylthiophenes are selective COX-2 inhibitors

Abstract A group of 3,4-diarylthiophenes containing either a sulfone or sulfonamide moiety were synthesized and tested for COX-1 and COX-2 inhibition. They are selective inhibitors of COX-2 and possess antiinflammatory activity in vivo .

4,5‐Diaryloxazole inhibitors of cyclooxygenase‐2 (COX‐2)

A series of methysulfonyl or sulfonamido substituted 4,5‐diaryloxazole were prepared and evaluated for their ability to inhibit the inducible form of cyclooxygenase (COX‐2) in vitro and in vivo. Several unique substitution patterns were identified that led to potent and selective inhibitors of COX‐2. In general, 2‐trifluoromethly‐4,5‐diaryloxazoles substituted with a methylsulfonyl or sulfonamido group were particularly potent inhibitors. One of the more potent compounds with a selectivity for COX‐2 of about 800 fold was 4b (SC‐299). SC‐299, a highly fluorescent molecule, may be useful for spectroscopic studies on preferential inhibitor binding to COX‐2.