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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. doi: 10.1016/j.bmcl.2009.09.050. Epub 2009 Sep 17.

Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.

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1
Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jack.scott@spcorp.com

Abstract

Vasopressin 1b (V1b) antagonists have been postulated as possible treatments for depression and anxiety. A novel series of potent and selective V1b antagonists has been identified starting from an in-house screen hit. The incorporation of a sulfonamide linker between a tetrahydroisoquinoline core and amino piperidine lead to the identification of a V1b antagonist with similar affinity for human and rat receptors. Further optimization of the right hand portion afforded potent V1b antagonists that possessed moderate to high selectivity over other receptors.

PMID:
19800231
DOI:
10.1016/j.bmcl.2009.09.050
[Indexed for MEDLINE]
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