title: Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists.
abstract: The SAR of a new series of tetrahydrocarbazole derivatives is described: the appropriate decoration of this template led to the identification of a new class of NPY-1 antagonists showing good in vitro potency and a promising in vivo pharmacokinetic profile in rat.
authors.affiliation: GlaxoSmithKline Medicines Research Centre, Via A. Fleming 4, 37135 Verona, Italy. rdf26781@gsk.com
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Riccardo
authors.initials: R
authors.lastname: Giovannini
authors.forename: Barbara
authors.initials: B
authors.lastname: Bertani
authors.forename: Manuela
authors.initials: M
authors.lastname: Borriello
authors.forename: Andrea
authors.initials: A
authors.lastname: Bozzoli
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: Colin P
authors.initials: CP
authors.lastname: Leslie
authors.forename: Angelo
authors.initials: A
authors.lastname: Pecunioso
authors.forename: Giovanna
authors.initials: G
authors.lastname: Rumboldt
authors.forename: Simone
authors.initials: S
authors.lastname: Spada
mesh_terms: D000818:Animals; D001682:Biological Availability; D016466:CHO Cells / Q000187:drug effects; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006224:Cricetinae; D003412:Cricetulus; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D002227:Carbazoles; D017476:Receptors, Neuropeptide Y; C097212:neuropeptide Y-Y1 receptor; C409925:1,2,3,4-tetrahydrocarbazole