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

doi:10.1016/j.bmcl.2005.03.045

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 language	English
Pages (from-to)	2579-2582
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	15
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2005.03.045
Publication status	Published - May 2005

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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

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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.",

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

year = "2005",

month = may,

doi = "10.1016/j.bmcl.2005.03.045",

language = "English",

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Wyatt, PG, Allen, MJ, Borthwick, AD, Davies, DE, Exall, AM, Hatley, RJD, Irving, WR, Livermore, DG, Miller, ND, Nerozzi, F, Sollis, SL & Szardenings, AK 2005, '2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: identification, stereochemistry and initial SAR', Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 10, pp. 2579-2582. https://doi.org/10.1016/j.bmcl.2005.03.045

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T1 - 2,5-Diketopiperazines as potent and selective oxytocin antagonists 1

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AU - Wyatt, Paul G.

AU - Allen, Michael J.

AU - Borthwick, Alan D.

AU - Davies, Dave E.

AU - Exall, Anne M.

AU - Hatley, Richard J. D.

AU - Irving, Wendy R.

AU - Livermore, David G.

AU - Miller, Neil D.

AU - Nerozzi, Fabrizio

AU - Sollis, Steve L.

AU - Szardenings, Anna Katrin

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AB - 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.

U2 - 10.1016/j.bmcl.2005.03.045

DO - 10.1016/j.bmcl.2005.03.045

M3 - Article

C2 - 15863320

SN - 1464-3405

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JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 10

ER -

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

Abstract

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