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Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: Novel, potent, and selective series of Vasopressin1b receptor antagonists

✍ Scribed by Roberto Arban; Federica Bianchi; Alberto Buson; Susanna Cremonesi; Romano Di Fabio; Gabriella Gentile; Fabrizio Micheli; Alessandra Pasquarello; Alfonso Pozzan; Luca Tarsi; Silvia Terreni; Federica Tonelli

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 496 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.037

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✦ Synopsis

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.

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