Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists

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

doi:10.1016/j.bmcl.2010.07.037

Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5044-9. doi: 10.1016/j.bmcl.2010.07.037. Epub 2010 Jul 14.

Authors

Roberto Arban¹, Federica Bianchi, Alberto Buson, Susanna Cremonesi, Romano Di Fabio, Gabriella Gentile, Fabrizio Micheli, Alessandra Pasquarello, Alfonso Pozzan, Luca Tarsi, Silvia Terreni, Federica Tonelli

Affiliation

¹ Department of Translational Biology, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Verona, Italy.

PMID: 20674355
DOI: 10.1016/j.bmcl.2010.07.037

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.

MeSH terms

Antidiuretic Hormone Receptor Antagonists*
Pyrazines / chemistry
Pyrazines / pharmacology*
Pyrroles / chemistry
Pyrroles / pharmacology*
Structure-Activity Relationship

Substances

Antidiuretic Hormone Receptor Antagonists
Pyrazines
Pyrroles