2,5-Diketopiperazines as potent and selective oxytocin antagonists 1:Identification, stereochemistry and initial SAR

Wyatt, Paul G, Allen, Michael J, Borthwick, Alan D, Davies, Dave E, Exall, Anne M, Hatley, Richard J D, Irving, Wendy R, Livermore, David G, Miller, Neil D, Nerozzi, Fabrizio, Sollis, Steve L and Szardenings, Anna Katrin (2005) 2,5-Diketopiperazines as potent and selective oxytocin antagonists 1:Identification, stereochemistry and initial SAR. Bioorganic & Medicinal Chemistry Letters, 15 (10). pp. 2579-82. ISSN 0960-894X

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Abstract

This paper covers efforts to discover orally active potent and selective oxytocin antagonists. Screening pooled libraries identified a novel series of 2,5-diketopiperazine derivatives with antagonist activity at the human oxytocin receptor. We report the initial structure-activity relationship investigations and the determination of the stereochemistry of the most potent compounds.

Item Type: Article
Uncontrolled Keywords: humans,piperazines,receptors, oxytocin,stereoisomerism,structure-activity relationship
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
Depositing User: Pure Connector
Date Deposited: 06 Jan 2014 14:56
Last Modified: 21 Apr 2020 22:38
URI: https://ueaeprints.uea.ac.uk/id/eprint/46735
DOI: 10.1016/j.bmcl.2005.03.045

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