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

DOI: 10.1016/S0960-894X(99)00560-0

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3187 - 3192 (1999)

Update date:2022-08-02

Topics:

Authors:

Lau, Cheuk K.

Brideau, Christine

Chan, Chi Chung

Charleson, Stella

Cromlish, Wanda A.

Ethier, Diane

Yves Gauthier, Jacques

Gordon, Robert

Guay, Jocelyne

Kargman, Stacia

Li, Chun-Sing

Prasit, Petpiboon

Riendeau, Denis

Therien, Michel

Visco, Denise M.

Xu, Lijing

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Article abstract of DOI:10.1016/S0960-894X(99)00560-0

A series of 3-heteroaryloxy-4-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.

Full text of DOI:10.1016/S0960-894X(99)00560-0

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