2. Academic Validation
  3. Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors

Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors

  • Bioorg Med Chem Lett. 1999 Nov 15;9(22):3187-92. doi: 10.1016/s0960-894x(99)00560-0.
C K Lau 1,  C Brideau,  C C Chan,  S Charleson,  W A Cromlish,  D Ethier,  J Y Gauthier,  R Gordon,  J Guay,  S Kargman,  C S Li,  P Prasit,  D Riendeau,  M Thérien,  D M Visco,  L Xu
Affiliations

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada.
PMID: 10576685 DOI: 10.1016/s0960-894x(99)00560-0
Abstract

A series of 3-heteroaryloxy4-phenyl-2-5H)-furanones were prepared and evaluated for their potency and selectivity as COX-2 inhibitors. This led to the identification of L-778,736 as a potent, orally active and selective inhibitor of the COX-2 enzyme.

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