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2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: Identification, stereochemistry and initial SAR |
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| Authors: | 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 Szardenings Anna Katrin |
| Affiliation: | Department of Medicinal Chemistry CVU UK, GlaxoSmithKline Research and Development Limited, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK. |
| 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. |
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