236747-80-1Relevant academic research and scientific papers
Structure-based design of COX-2 selectivity into flurbiprofen
Bayly, Christopher I.,Black, W. Cameron,Leger, Serge,Ouimet, Nathalie,Ouellet, Marc,Percival, M. David
, p. 307 - 312 (1999)
Comparative computer modeling of the X-ray crystal structures of cyclooxygenase isoforms COX-1 and COX-2 has led to the design of COX-2 selectivity into the nonselective inhibitor flurbiprofen. The COX-2 modeling was based on a postulated binding mode for flurbiprofen and took advantage of a small alcove in the COX-2 active site created by different positions of the Leu384 sidechain between COX-1 and COX-2. The design hypothesis was tested by synthesis and biological assay of a series of flurbiprofen analogs, culminating in the discovery of several inhibitors having up to 78-fold selectivity for COX-2 over COX-1.
BIARYL-ACETIC ACID DERIVATIVES AND THEIR USE AS COX-2 INHIBITORS
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Page/Page column 15, (2010/02/03)
The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: and include pharmaceutically acceptable salts and esters thereof.
