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Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors |
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| Authors: | Lau C K Brideau C Chan C C Charleson S Cromlish W A Ethier D Gauthier J Y Gordon R Guay J Kargman S Li C S Prasit P Riendeau D Thérien M Visco D M Xu L |
| Affiliation: | Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada. |
| 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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