title: SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor.
abstract: Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanon e), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, Québec, Canada.
authors.forename: Y
authors.initials: Y
authors.lastname: Leblanc
authors.forename: P
authors.initials: P
authors.lastname: Roy
authors.forename: S
authors.initials: S
authors.lastname: Boyce
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: R
authors.initials: R
authors.lastname: Gordon
authors.forename: E
authors.initials: E
authors.lastname: Grimm
authors.forename: J
authors.initials: J
authors.lastname: Guay
authors.forename: S
authors.initials: S
authors.lastname: Léger
authors.forename: C S
authors.initials: CS
authors.lastname: Li
authors.forename: D
authors.initials: D
authors.lastname: Riendeau
authors.forename: D
authors.initials: D
authors.lastname: Visco
authors.forename: Z
authors.initials: Z
authors.lastname: Wang
authors.forename: J
authors.initials: J
authors.lastname: Webb
authors.forename: L J
authors.initials: LJ
authors.lastname: Xu
authors.forename: P
authors.initials: P
authors.lastname: Prasit
mesh_terms: D000284:Administration, Oral; D000818:Animals; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D007527:Isoenzymes / Q000187:drug effects / Q000378:metabolism*; D008253:Macaca mulatta; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D012453:Saimiri; D013329:Structure-Activity Relationship; D020298:U937 Cells
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases