title: 2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.
abstract: Biaryl amides were discovered as novel and subtype selective M(1) muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M(1) agonist potency and intrinsic activity, and subtype selectivity for M(1) over M(2-5), are described.
authors.affiliation: Discovery Research and Centers of Excellence for Drug Discovery, GlaxoSmithKline, Collegeville, PA 19426, USA. torqux@yahoo.com
authors.forename: Brian
authors.initials: B
authors.lastname: Budzik
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Garzya
authors.forename: Dongchuan
authors.initials: D
authors.lastname: Shi
authors.forename: James J
authors.initials: JJ
authors.lastname: Foley
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Rivero
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Langmead
authors.forename: Jeannette
authors.initials: J
authors.lastname: Watson
authors.forename: Zining
authors.initials: Z
authors.lastname: Wu
authors.forename: Ian T
authors.initials: IT
authors.lastname: Forbes
authors.forename: Jian
authors.initials: J
authors.lastname: Jin
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D055808:Drug Discovery; D006841:Hydrocarbons, Aromatic / Q000138:chemical synthesis* / Q000494:pharmacology; D015394:Molecular Structure; D043643:Receptor, Muscarinic M1 / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D006841:Hydrocarbons, Aromatic; D043643:Receptor, Muscarinic M1