Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.
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.
Arban
Roberto
R
Department of Translational Biology, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Verona, Italy.
Bianchi
Federica
F
Buson
Alberto
A
Cremonesi
Susanna
S
Di Fabio
Romano
R
Gentile
Gabriella
G
Micheli
Fabrizio
F
Pasquarello
Alessandra
A
Pozzan
Alfonso
A
Tarsi
Luca
L
Terreni
Silvia
S
Tonelli
Federica
F
D065092:Antidiuretic Hormone Receptor Antagonists; D011719:Pyrazines / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D065092:Antidiuretic Hormone Receptor Antagonists; D011719:Pyrazines; D011758:Pyrroles