title: Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.
abstract: A series of 8-azabicyclo[3.2.1]octane amine hNK1 antagonists has been investigated and structure-activity relationships of the benzylamine and 6-exo substituents described. Acidic substituents at C6 give a series of high affinity compounds for hNK1 with selectivity over the hERG channel.
authors.affiliation: Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. christopher_thomson@merck.com
authors.forename: Christopher G
authors.initials: CG
authors.lastname: Thomson
authors.forename: Emma
authors.initials: E
authors.lastname: Carlson
authors.forename: Gary G
authors.initials: GG
authors.lastname: Chicchi
authors.forename: Janusz J
authors.initials: JJ
authors.lastname: Kulagowski
authors.forename: Marc M
authors.initials: MM
authors.lastname: Kurtz
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Swain
authors.forename: Kwei-Lan C
authors.initials: KL
authors.lastname: Tsao
authors.forename: Alan
authors.initials: A
authors.lastname: Wheeldon
mesh_terms: D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D008968:Molecular Conformation; D064729:Neurokinin-1 Receptor Antagonists; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: C509738:8-azabicyclo(3.2.1)octane benzylamine; D001372:Aza Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D064729:Neurokinin-1 Receptor Antagonists