title: 5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers.
abstract: Structure-activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described. The 4-cyano-5-alkyl ethers were found to have excellent potency and selectivity, whereas the 5-thioethers were potent but less selective than the ether analogs in a canine whole blood (CWB) COX-2 assay.
authors.affiliation: Veterinary Medicine Research and Development, Pfizer Inc., Groton, CT 06340, USA. subas.m.sakya@pfizer.com
authors.forename: Subas M
authors.initials: SM
authors.lastname: Sakya
authors.forename: Hengmiao
authors.initials: H
authors.lastname: Cheng
authors.forename: Kristin M
authors.initials: KM
authors.lastname: Lundy Demello
authors.forename: Andrei
authors.initials: A
authors.lastname: Shavnya
authors.forename: Martha L
authors.initials: ML
authors.lastname: Minich
authors.forename: Bryson
authors.initials: B
authors.lastname: Rast
authors.forename: Jason
authors.initials: J
authors.lastname: Dutra
authors.forename: Chao
authors.initials: C
authors.lastname: Li
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Rafka
authors.forename: David A
authors.initials: DA
authors.lastname: Koss
authors.forename: Jin
authors.initials: J
authors.lastname: Li
authors.forename: Burton H
authors.initials: BH
authors.lastname: Jaynes
authors.forename: Carl B
authors.initials: CB
authors.lastname: Ziegler
authors.forename: Donald W
authors.initials: DW
authors.lastname: Mann
authors.forename: Carol F
authors.initials: CF
authors.lastname: Petras
authors.forename: Scott B
authors.initials: SB
authors.lastname: Seibel
authors.forename: Annette M
authors.initials: AM
authors.lastname: Silvia
authors.forename: David M
authors.initials: DM
authors.lastname: George
authors.forename: Anne
authors.initials: A
authors.lastname: Hickman
authors.forename: Michelle L
authors.initials: ML
authors.lastname: Haven
authors.forename: Michael P
authors.initials: MP
authors.lastname: Lynch
mesh_terms: D000478:Alkylation; D000818:Animals; D051546:Cyclooxygenase 2 / Q000378:metabolism*; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004285:Dogs; D004987:Ethers / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011720:Pyrazoles / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry*
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D004987:Ethers; D011720:Pyrazoles; D013438:Sulfhydryl Compounds; D051546:Cyclooxygenase 2