title: Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship.
abstract: Series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and in IL-1beta stimulated synovial fibroblasts. The 2-amino-5-chloropyridine-4-carboxamides were identified as the most potent inhibitors with improved cellular activity.
authors.affiliation: Department of Medicinal Chemistry, Pfizer Inc, 700 Chesterfield Parkway West, St Louis, MO 63017, United States. dominique.bonafoux@abbott.com
authors.forename: Dominique F
authors.initials: DF
authors.lastname: Bonafoux
authors.forename: Sheri L
authors.initials: SL
authors.lastname: Bonar
authors.forename: Michael
authors.initials: M
authors.lastname: Clare
authors.forename: Ann M
authors.initials: AM
authors.lastname: Donnelly
authors.forename: Jeanette L
authors.initials: JL
authors.lastname: Glaenzer
authors.forename: Julia A
authors.initials: JA
authors.lastname: Guzova
authors.forename: He
authors.initials: H
authors.lastname: Huang
authors.forename: Nandidni N
authors.initials: NN
authors.lastname: Kishore
authors.forename: Francis J
authors.initials: FJ
authors.lastname: Koszyk
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Lennon
authors.forename: Adam
authors.initials: A
authors.lastname: Libby
authors.forename: Sumathy
authors.initials: S
authors.lastname: Mathialagan
authors.forename: David S
authors.initials: DS
authors.lastname: Oburn
authors.forename: Sharon A
authors.initials: SA
authors.lastname: Rouw
authors.forename: Cynthia D
authors.initials: CD
authors.lastname: Sommers
authors.forename: Catherine S
authors.initials: CS
authors.lastname: Tripp
authors.forename: Lori J
authors.initials: LJ
authors.lastname: Vanella
authors.forename: Richard
authors.initials: R
authors.lastname: Weier
authors.forename: Serge G
authors.initials: SG
authors.lastname: Wolfson
authors.forename: Horng-Chih
authors.initials: HC
authors.lastname: Huang
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000595:Amino Acid Sequence; D000632:Aminopyrine / Q000737:chemistry* / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology*; D001172:Arthritis, Rheumatoid / Q000188:drug therapy; D005347:Fibroblasts / Q000187:drug effects / Q000276:immunology; D006801:Humans; D051550:I-kappa B Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020672:I-kappa B Proteins / Q000737:chemistry; D053583:Interleukin-1beta / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017746:Joint Capsule / Q000166:cytology; D008969:Molecular Sequence Data; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000893:Anti-Inflammatory Agents; C083487:I kappa B beta protein; D020672:I-kappa B Proteins; D053583:Interleukin-1beta; D000632:Aminopyrine; D051550:I-kappa B Kinase