Abstract
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.
Original language | English |
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Pages (from-to) | 199-208 |
Number of pages | 10 |
Journal | Medicinal Research Reviews |
Volume | 19 |
Issue number | 3 |
DOIs | |
State | Published - 1999 |
Keywords
- Anti-inflammatory
- COX-2
- COX-2 inhibitors
- Cyclooxygenase-2
- Diaryloxazole
- Inflammation