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

Paul G Wyatt, Michael J Allen, Alan D Borthwick, Dave E Davies, Anne M Exall, Richard J D Hatley, Wendy R Irving, David G Livermore, Neil D Miller, Fabrizio Nerozzi, Steve L Sollis, Anna Katrin Szardenings

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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.
Original languageEnglish
Pages (from-to)2579-82
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Issue number10
Publication statusPublished - 16 May 2005


  • Humans
  • Piperazines
  • Receptors, Oxytocin
  • Stereoisomerism
  • Structure-Activity Relationship

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