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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    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.
    Original languageEnglish
    Pages (from-to)2579-2582
    Number of pages4
    JournalBioorganic & Medicinal Chemistry Letters
    Volume15
    Issue number10
    DOIs
    Publication statusPublished - May 2005

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  • Cite this

    Wyatt, P. G., Allen, M. J., Borthwick, A. D., Davies, D. E., Exall, A. M., Hatley, R. J. D., Irving, W. R., Livermore, D. G., Miller, N. D., Nerozzi, F., Sollis, S. L., & Szardenings, A. K. (2005). 2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: identification, stereochemistry and initial SAR. Bioorganic & Medicinal Chemistry Letters, 15(10), 2579-2582. https://doi.org/10.1016/j.bmcl.2005.03.045