title: New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.
abstract: The synthesis and SAR of a new series of potent and selective dopamine D(3) receptor antagonists is reported. The introduction of a tricyclic [h]-fused benzazepine moiety on the recently disclosed scaffold of 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines is reported. A full rat pharmacokinetic characterization is also reported.
authors.affiliation: GlaxoSmithKline, Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy. fm20244@gsk.com
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Micheli
authors.forename: Giorgio
authors.initials: G
authors.lastname: Bonanomi
authors.forename: Simone
authors.initials: S
authors.lastname: Braggio
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Capelli
authors.forename: Paolo
authors.initials: P
authors.lastname: Celestini
authors.forename: Federica
authors.initials: F
authors.lastname: Damiani
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Daniele
authors.initials: D
authors.lastname: Donati
authors.forename: Stefania
authors.initials: S
authors.lastname: Gagliardi
authors.forename: Gabriella
authors.initials: G
authors.lastname: Gentile
authors.forename: Dieter
authors.initials: D
authors.lastname: Hamprecht
authors.forename: Marcella
authors.initials: M
authors.lastname: Petrone
authors.forename: Stefano
authors.initials: S
authors.lastname: Radaelli
authors.forename: Giovanna
authors.initials: G
authors.lastname: Tedesco
authors.forename: Silvia
authors.initials: S
authors.lastname: Terreni
authors.forename: Angela
authors.initials: A
authors.lastname: Worby
authors.forename: Christian
authors.initials: C
authors.lastname: Heidbreder
mesh_terms: D000818:Animals; D001552:Benzazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D015394:Molecular Structure; D051381:Rats; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001552:Benzazepines; D018492:Dopamine Antagonists; D050637:Receptors, Dopamine D3