title: Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.
abstract: Novel series of pyrrole-pyrazinone and pyrazole-pyrazinone have been identified as potent and selective Vasopressin(1b) receptor antagonists. Exploration of the substitution pattern around the core of these templates allowed generation of compounds with high inhibitory potency at the Vasopressin(1b) receptor, including examples that showed good selectivity with respect to Vasopressin(1a), Vasopressin(2), and Oxytocin receptor subtypes.
authors.affiliation: Department of Translational Biology, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Verona, Italy.
authors.forename: Roberto
authors.initials: R
authors.lastname: Arban
authors.forename: Federica
authors.initials: F
authors.lastname: Bianchi
authors.forename: Alberto
authors.initials: A
authors.lastname: Buson
authors.forename: Susanna
authors.initials: S
authors.lastname: Cremonesi
authors.forename: Romano
authors.initials: R
authors.lastname: Di Fabio
authors.forename: Gabriella
authors.initials: G
authors.lastname: Gentile
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Micheli
authors.forename: Alessandra
authors.initials: A
authors.lastname: Pasquarello
authors.forename: Alfonso
authors.initials: A
authors.lastname: Pozzan
authors.forename: Luca
authors.initials: L
authors.lastname: Tarsi
authors.forename: Silvia
authors.initials: S
authors.lastname: Terreni
authors.forename: Federica
authors.initials: F
authors.lastname: Tonelli
mesh_terms: D065092:Antidiuretic Hormone Receptor Antagonists; D011719:Pyrazines / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D065092:Antidiuretic Hormone Receptor Antagonists; D011719:Pyrazines; D011758:Pyrroles