title: Novel carbazole derivatives as NPY Y1 antagonists.
abstract: The synthesis of a series of carbazole derivatives and their SAR at the NPY Y1 receptor is described. Modulation of physicochemical properties by appropriate decoration led to the identification of a high-affinity NPY Y1 antagonist that shows high brain penetration and modest oral bioavailability.
authors.affiliation: GlaxoSmithKline Medicines Research Centre, Via A. Fleming 4, Verona 37135, Italy. colin.p.leslie@gsk.com
authors.forename: Colin P
authors.initials: CP
authors.lastname: Leslie
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Francesca
authors.initials: F
authors.lastname: Bonetti
authors.forename: Manuela
authors.initials: M
authors.lastname: Borriello
authors.forename: Simone
authors.initials: S
authors.lastname: Braggio
authors.forename: Giovanna
authors.initials: G
authors.lastname: Dal Forno
authors.forename: Daniele
authors.initials: D
authors.lastname: Donati
authors.forename: Alessandro
authors.initials: A
authors.lastname: Falchi
authors.forename: Damiano
authors.initials: D
authors.lastname: Ghirlanda
authors.forename: Riccardo
authors.initials: R
authors.lastname: Giovannini
authors.forename: Francesca
authors.initials: F
authors.lastname: Pavone
authors.forename: Angelo
authors.initials: A
authors.lastname: Pecunioso
authors.forename: Giorgio
authors.initials: G
authors.lastname: Pentassuglia
authors.forename: Domenica A
authors.initials: DA
authors.lastname: Pizzi
authors.forename: Giovanna
authors.initials: G
authors.lastname: Rumboldt
authors.forename: Luigi
authors.initials: L
authors.lastname: Stasi
mesh_terms: D000818:Animals; D001682:Biological Availability; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D016466:CHO Cells; D002227:Carbazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006224:Cricetinae; D003412:Cricetulus; D006207:Half-Life; D007202:Indicators and Reagents; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D002227:Carbazoles; D007202:Indicators and Reagents; D017476:Receptors, Neuropeptide Y; C097212:neuropeptide Y-Y1 receptor