Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 1999 May;19(3):199-208.
doi: 10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co;2-7.

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

J J Talley  1 , S R Bertenshaw, D L Brown, J S Carter, M J Graneto, C M Koboldt, J L Masferrer, B H Norman, D J Rogier Jr, B S Zwwifel, K Seibert
Affiliations
Review

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

J J Talley et al. Med Res Rev. 1999 May.

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.

PubMed Disclaimer

MeSH terms

LinkOut - more resources