2. Academic Validation
  3. 2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors

2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors

  • J Med Chem. 1999 Apr 8;42(7):1274-81. doi: 10.1021/jm980642l.
W C Black 1,  C Brideau,  C C Chan,  S Charleson,  N Chauret,  D Claveau,  D Ethier,  R Gordon,  G Greig,  J Guay,  G Hughes,  P Jolicoeur,  Y Leblanc,  D Nicoll-Griffith,  N Ouimet,  D Riendeau,  D Visco,  Z Wang,  L Xu,  P Prasit
Affiliations

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, P.O. Box 1005, Pointe-Claire-Dorval, Québec, Canada H9R 4P8, and Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.
PMID: 10197970 DOI: 10.1021/jm980642l
Abstract

Cyclopentenones containing a 4-(methylsulfonyl)phenyl group in the 3-position and a phenyl ring in the 2-position are selective inhibitors of cyclooxygenase-2 (COX-2). The selectivity for COX-2 over COX-1 is dramatically improved by substituting the 2-phenyl group with halogens in the meta position or by replacing the phenyl ring with a 2- or 3-pyridyl ring. Thus the 3,5-difluorophenyl derivative 7 (L-776,967) and the 3-pyridyl derivative 13 (L-784,506) are particularly interesting as potential antiinflammatory agents with reduced side-effect profiles. Both exhibit good oral bioavailability and are potent in standard models of pain, fever, and inflammation yet have a much reduced effect on the GI integrity of rats compared to standard nonsteroidal antiflammatory drugs.

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