title: A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.
abstract: By inserting an oxygen link between the 3-fluorophenyl and the lactone ring of 5,5-dimethyl-3-(3fluorophenyl)-4-(4-methanesulfonylphenyl)-2 (5H)-furanone 1 (DFU), analogs with enhanced in vitro COX-2 inhibitory potency as well as in vivo potency in models of inflammation were obtained.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, Pointe-Clarie-Dorval, Quebec, Canada.
authors.forename: C S
authors.initials: CS
authors.lastname: Li
authors.forename: W C
authors.initials: WC
authors.lastname: Black
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: Claveau
authors.forename: J Y
authors.initials: JY
authors.lastname: Gauthier
authors.forename: R
authors.initials: R
authors.lastname: Gordon
authors.forename: G
authors.initials: G
authors.lastname: Greig
authors.forename: E
authors.initials: E
authors.lastname: Grimm
authors.forename: J
authors.initials: J
authors.lastname: Guay
authors.forename: C K
authors.initials: CK
authors.lastname: Lau
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: E
authors.initials: E
authors.lastname: Wong
authors.forename: L
authors.initials: L
authors.lastname: Xu
authors.forename: P
authors.initials: P
authors.lastname: Prasit
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000494:pharmacology; D016466:CHO Cells; D006224:Cricetinae; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D005663:Furans / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D007527:Isoenzymes / Q000187:drug effects*; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: C106876:5,5-dimethyl-3-(3-fluorophenyl)-4-(4-methylsulfonyl)phenyl-2(5H)-furanone; D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D005663:Furans; D007527:Isoenzymes; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases