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

Novel series of pyrrole-pyrazinone and pyrazole-pyrazinone have been identified as potent and selective Vasopressin1b receptor antagonists. Exploration of the substitution pattern around the core of these templates allowed generation of compounds with high inhibitory potency at the Vasopressin1b receptor, including examples that showed good selectivity with respect to Vasopressin1a, Vasopressin2, and Oxytocin receptor subtypes.

Graphical abstractNovel series of pyrrole-pyrazinone and pyrazole-pyrazinone have been identified as potent and selective Vasopressin1b receptor antagonists. Exploration of the substitution pattern around the core of these templates allowed generation of compounds with high inhibitory potency at Vasopressin1b receptor including examples that showed good selectivity with respect to Vasopressin1a, Vasopressin2, and Oxytocin receptors subtype.Figure optionsDownload full-size imageDownload as PowerPoint slide