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. 2011 Jun 15;21(12):3828-31.
doi: 10.1016/j.bmcl.2011.03.012. Epub 2011 Mar 6.

Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties

Thorsten Oost  1 , Gisela Backfisch, Swati Bhowmik, Marcel M van Gaalen, Hervé Geneste, Wilfried Hornberger, Wilfried Lubisch, Astrid Netz, Liliane Unger, Wolfgang Wernet
Affiliations

Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties

Thorsten Oost et al. Bioorg Med Chem Lett. .

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.

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