title: 2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.
abstract: A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and COX-2. Optimum COX-2 activity is observed by introduction of a substituent at C5 of the central pyridine. 5- Chloro-3-(4-methylsulfonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine 33 was identified as the optimum compound in this series.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada.
authors.forename: R W
authors.initials: RW
authors.lastname: Friesen
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: D
authors.initials: D
authors.lastname: Deschênes
authors.forename: D
authors.initials: D
authors.lastname: Dubé
authors.forename: D
authors.initials: D
authors.lastname: Ethier
authors.forename: R
authors.initials: R
authors.lastname: Fortin
authors.forename: J Y
authors.initials: JY
authors.lastname: Gauthier
authors.forename: Y
authors.initials: Y
authors.lastname: Girard
authors.forename: R
authors.initials: R
authors.lastname: Gordon
authors.forename: G M
authors.initials: GM
authors.lastname: Greig
authors.forename: D
authors.initials: D
authors.lastname: Riendeau
authors.forename: C
authors.initials: C
authors.lastname: Savoie
authors.forename: Z
authors.initials: Z
authors.lastname: Wang
authors.forename: E
authors.initials: E
authors.lastname: Wong
authors.forename: D
authors.initials: D
authors.lastname: Visco
authors.forename: L J
authors.initials: LJ
authors.lastname: Xu
authors.forename: R N
authors.initials: RN
authors.lastname: Young
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D016466:CHO Cells / Q000187:drug effects / Q000201:enzymology; D006224:Cricetinae; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004487:Edema / Q000188:drug therapy; D006801:Humans; D007527:Isoenzymes / Q000187:drug effects*; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D011725:Pyridines; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; C496513:Ptgs1 protein, rat