Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: Novel,potent, and selective series of Vasopressin1b receptor antagonists |
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| Authors: | 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 |
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| Affiliation: | 1. Department of Medicinal Chemistry, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Via A Fleming 4, 37135 Verona, Italy;2. Computational and Structural Chemistry, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Via A Fleming 4, 37135 Verona, Italy;3. Department of Translational Biology, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Via A Fleming 4, 37135 Verona, Italy;4. PCDD&ET, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Via A Fleming 4, 37135 Verona, Italy;5. Screening and Compound Profiling, GlaxoSmithKline, Neuroscience Centre of Excellence for Drug Discovery, Via A Fleming 4, 37135 Verona, Italy |
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| Abstract: | 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. |
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