title: Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists.
abstract: A novel series of 1,2,4-triazol-3-yl-azabicyclo[3.1.0]hexanes with high affinity and selectivity for the DA D(3) receptor and excellent pharmacokinetic profiles was recently reported. We also recently discussed the role of the linker associated with the triazole moiety. In this manuscript, we are reporting a detailed exploration of the region of the receptor interacting with the amine terminus of the scaffold wherein SAR and developability data associated with these novel templates was undertaken.
authors.affiliation: Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy. fabrizio.micheli@aptuit.com
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Micheli
authors.forename: Luca
authors.initials: L
authors.lastname: Arista
authors.forename: Barbara
authors.initials: B
authors.lastname: Bertani
authors.forename: Simone
authors.initials: S
authors.lastname: Braggio
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Capelli
authors.forename: Susanna
authors.initials: S
authors.lastname: Cremonesi
authors.forename: Romano
authors.initials: R
authors.lastname: Di-Fabio
authors.forename: Giacomo
authors.initials: G
authors.lastname: Gelardi
authors.forename: Gabriella
authors.initials: G
authors.lastname: Gentile
authors.forename: Carla
authors.initials: C
authors.lastname: Marchioro
authors.forename: Alessandra
authors.initials: A
authors.lastname: Pasquarello
authors.forename: Stefano
authors.initials: S
authors.lastname: Provera
authors.forename: Giovanna
authors.initials: G
authors.lastname: Tedesco
authors.forename: Luca
authors.initials: L
authors.lastname: Tarsi
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; D053961:Azabicyclo Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016466:CHO Cells; D020134:Catalytic Domain; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D066298:In Vitro Techniques; D008862:Microsomes, Liver / Q000378:metabolism; D008958:Models, Molecular; D011869:Radioligand Assay; D051381:Rats; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D053961:Azabicyclo Compounds; D050637:Receptors, Dopamine D3; D014230:Triazoles