title: Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.
abstract: In the course of our research program to develop novel muscarinic receptor antagonists for the treatment of COPD, new tropane carbamate derivatives were identified as potent anti-muscarinic agents. The synthesis, structure-activity relationships and pharmacological evaluation that led to the identification of compound 5o, are described.
authors.affiliation: GlaxoSmithkline, 709 Swedeland Road, King of Prussia, PA 19406, USA. dramane.i.laine@gsk.com
authors.forename: Dramane I
authors.initials: DI
authors.lastname: Lainé
authors.forename: Haibo
authors.initials: H
authors.lastname: Xie
authors.forename: Noémie
authors.initials: N
authors.lastname: Buffet
authors.forename: James J
authors.initials: JJ
authors.lastname: Foley
authors.forename: Peter
authors.initials: P
authors.lastname: Buckley
authors.forename: Edward F
authors.initials: EF
authors.lastname: Webb
authors.forename: Katherine L
authors.initials: KL
authors.lastname: Widdowson
authors.forename: Michael R
authors.initials: MR
authors.lastname: Palovich
authors.forename: Kristen E
authors.initials: KE
authors.lastname: Belmonte
mesh_terms: D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001993:Bronchodilator Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002219:Carbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D018727:Muscarinic Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D029424:Pulmonary Disease, Chronic Obstructive / Q000628:therapy; D011976:Receptors, Muscarinic / Q000187:drug effects*; D014326:Tropanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D019086:Bridged Bicyclo Compounds, Heterocyclic; D001993:Bronchodilator Agents; D002219:Carbamates; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic; D014326:Tropanes