Title of article :
2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: identification, stereochemistry and initial SAR
Author/Authors :
Paul G. Wyatt، نويسنده , , Michael J. Allen، نويسنده , , Alan D. Borthwick، نويسنده , , Dave E. Davies، نويسنده , , Anne M. Exall، نويسنده , , Richard J.D. Hatley، نويسنده , , Wendy R. Irving، نويسنده , , David G. Livermore، نويسنده , , Neil D. Miller، نويسنده , , Fabrizio Nerozzi، نويسنده , , Steve L. Sollis، نويسنده , , Anna Katrin Szardenings، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
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 :
Antagonists , 2 , 5-Diketopiperidines , screening , Pooled libraries , Solid phase , Ugi reaction , Structure–activity relationships , Oxytocin , Oxytocin receptor , Preterm birth , Unencoded libraries
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
