title: Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists.
abstract: A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modification of a screening hit. Structure-activity relationships and efforts undertaken to achieve a favourable pharmacokinetic profile in rat are described.
authors.affiliation: GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicines Research Centre, Verona, Italy. matteo.2.biagetti@gsk.com
authors.forename: Matteo
authors.initials: M
authors.lastname: Biagetti
authors.forename: Colin Philip
authors.initials: CP
authors.lastname: Leslie
authors.forename: Angelica
authors.initials: A
authors.lastname: Mazzali
authors.forename: Catia
authors.initials: C
authors.lastname: Seri
authors.forename: Domenica Antonia
authors.initials: DA
authors.lastname: Pizzi
authors.forename: Jonathan
authors.initials: J
authors.lastname: Bentley
authors.forename: Thorsten
authors.initials: T
authors.lastname: Genski
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Laura
authors.initials: L
authors.lastname: Zonzini
authors.forename: Laura
authors.initials: L
authors.lastname: Caberlotto
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D053961:Azabicyclo Compounds / Q000737:chemistry*; D002460:Cell Line; D006801:Humans; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D053961:Azabicyclo Compounds; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor