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

TY - JOUR

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

T2 - identification, stereochemistry and initial SAR

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

PY - 2005/5

Y1 - 2005/5

N2 - 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.

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

VL - 15

SP - 2579

EP - 2582

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 10

ER -