Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: Novel, potent, and selective series of Vasopressin(1b) receptor antagonists.
Bioorganic & medicinal chemistry letters 2010 Jul 14; In press
Arban R, Bianchi F, Buson A, Cremonesi S, Fabio R RD, Gentile G, Micheli F, Pasquarello A, Pozzan A, Tarsi L, Terreni S, Tonelli F
Department of Translational Biology, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Via A Fleming 4, 37135 Verona, Italy.
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.
Keywords: Vasopressin Oxytocin