2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: Identification, stereochemistry and initial SAR.
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.
Wyatt
Paul G
PG
Department of Medicinal Chemistry CVU UK, GlaxoSmithKline Research and Development Limited, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK.
Allen
Michael J
MJ
Borthwick
Alan D
AD
Davies
Dave E
DE
Exall
Anne M
AM
Hatley
Richard J D
RJ
Irving
Wendy R
WR
Livermore
David G
DG
Miller
Neil D
ND
Nerozzi
Fabrizio
F
Sollis
Steve L
SL
Szardenings
Anna Katrin
AK
D006801:Humans; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology*; D018045:Receptors, Oxytocin / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D010879:Piperazines; D018045:Receptors, Oxytocin