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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 
ORCID: https://orcid.org/0000-0002-9856-3703, 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
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 |
| UEA Research Groups: | Faculty of Medicine and Health Sciences > Research Groups > Epidemiology and Public Health Faculty of Medicine and Health Sciences > Research Groups > Public Health and Health Services Research (former - to 2023) |
| Depositing User: | Pure Connector |
| Date Deposited: | 06 Jan 2014 14:56 |
| Last Modified: | 24 Oct 2022 05:47 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/46735 |
| DOI: | 10.1016/j.bmcl.2005.03.045 |
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