Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
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.
Lau, CK; Brideau, C; Chan, CC; Charleson, S; Cromlish, WA; Ethier, D; Gauthier, JY; Gordon, R; Guay, J; Kargman, S; Li, CS; Prasit, P; Riendeau, D; Thérien, M; Visco, DM; Xu, L
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