title: Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
abstract: We describe herein the medicinal chemistry approach which led to the discovery of a novel pyridine-3-carboxamide series of CB(2) receptor agonists. The SAR of this new template was evaluated and culminated in the identification of analogue 14a which demonstrated efficacy in an in vivo model of inflammatory pain.
authors.affiliation: GlaxoSmithKline PLC, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK. bill.mitchell777@tiscali.co.uk
authors.forename: William L
authors.initials: WL
authors.lastname: Mitchell
authors.forename: Gerard M P
authors.initials: GM
authors.lastname: Giblin
authors.forename: Alan
authors.initials: A
authors.lastname: Naylor
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Eatherton
authors.forename: Brian P
authors.initials: BP
authors.lastname: Slingsby
authors.forename: Anthony D
authors.initials: AD
authors.lastname: Rawlings
authors.forename: Karamjit S
authors.initials: KS
authors.lastname: Jandu
authors.forename: Carl P
authors.initials: CP
authors.lastname: Haslam
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Brown
authors.forename: Paul
authors.initials: P
authors.lastname: Goldsmith
authors.forename: Nick M
authors.initials: NM
authors.lastname: Clayton
authors.forename: Alex W
authors.initials: AW
authors.lastname: Wilson
authors.forename: Iain P
authors.initials: IP
authors.lastname: Chessell
authors.forename: Richard H
authors.initials: RH
authors.lastname: Green
authors.forename: Andrew R
authors.initials: AR
authors.lastname: Whittington
authors.forename: Ian D
authors.initials: ID
authors.lastname: Wall
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D000698:Analgesia / Q000379:methods; D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D004195:Disease Models, Animal; D055808:Drug Discovery / Q000379:methods; D007249:Inflammation; D010146:Pain / Q000188:drug therapy; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000700:Analgesics; D011725:Pyridines; D043885:Receptor, Cannabinoid, CB2