title: Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
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.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada.
authors.forename: C K
authors.initials: CK
authors.lastname: Lau
authors.forename: C
authors.initials: C
authors.lastname: Brideau
authors.forename: C C
authors.initials: CC
authors.lastname: Chan
authors.forename: S
authors.initials: S
authors.lastname: Charleson
authors.forename: W A
authors.initials: WA
authors.lastname: Cromlish
authors.forename: D
authors.initials: D
authors.lastname: Ethier
authors.forename: J Y
authors.initials: JY
authors.lastname: Gauthier
authors.forename: R
authors.initials: R
authors.lastname: Gordon
authors.forename: J
authors.initials: J
authors.lastname: Guay
authors.forename: S
authors.initials: S
authors.lastname: Kargman
authors.forename: C S
authors.initials: CS
authors.lastname: Li
authors.forename: P
authors.initials: P
authors.lastname: Prasit
authors.forename: D
authors.initials: D
authors.lastname: Riendeau
authors.forename: M
authors.initials: M
authors.lastname: Thérien
authors.forename: D M
authors.initials: DM
authors.lastname: Visco
authors.forename: L
authors.initials: L
authors.lastname: Xu
mesh_terms: D000818:Animals; D001682:Biological Availability; D016466:CHO Cells; D006224:Cricetinae; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D005663:Furans / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D007527:Isoenzymes / Q000187:drug effects*; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects*; D011725:Pyridines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D005663:Furans; D007527:Isoenzymes; C401741:L 778736; D008565:Membrane Proteins; D011725:Pyridines; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases