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

Research output: Contribution to journal › Article › peer-review

71 Citations (Scopus)

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)	2579-82
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 - 16 May 2005

Keywords

Humans
Piperazines
Receptors, Oxytocin
Stereoisomerism
Structure-Activity Relationship

Access to Document

10.1016/j.bmcl.2005.03.045

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), 2579-82. https://doi.org/10.1016/j.bmcl.2005.03.045

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. / 2,5-Diketopiperazines as potent and selective oxytocin antagonists 1 : Identification, stereochemistry and initial SAR. In: Bioorganic & Medicinal Chemistry Letters. 2005 ; Vol. 15, No. 10. pp. 2579-82.

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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.",

keywords = "Humans, Piperazines, Receptors, Oxytocin, Stereoisomerism, Structure-Activity Relationship",

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}",

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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. 2579-82. https://doi.org/10.1016/j.bmcl.2005.03.045

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

In: Bioorganic & Medicinal Chemistry Letters, Vol. 15, No. 10, 16.05.2005, p. 2579-82.

Research output: Contribution to journal › Article › peer-review

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