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Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties
Authors:Oost Thorsten  Backfisch Gisela  Bhowmik Swati  van Gaalen Marcel M  Geneste Hervé  Hornberger Wilfried  Lubisch Wilfried  Netz Astrid  Unger Liliane  Wernet Wolfgang
Institution:Abbott, Neuroscience Discovery, D-67008 Ludwigshafen, Germany
Abstract:Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amine moiety to the northern phenyl ring resulted in potent and selective V1b receptor antagonists with improved metabolic stability and improved pharmacokinetic properties in rat. Compound 18c was found to be efficacious in a rat model of anti-depressant activity.
Keywords:Vasopressin 1b  V1b  SSR149415  Oxindole  Metabolic stability
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