Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.
The paper covers continuing efforts to discover novel, potent and selective oxytocin antagonists. Further benzofuran derivatives with potent oxytocin antagonist activity and good pharmacokinetic parameters are reported. Efforts to improve the in vivo activity of the series are described.
Wyatt
Paul G
PG
Department of Medicinal Chemistry, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, Herts, UK.
Allen
Michael J
MJ
Chilcott
Josie
J
Gardner
Christopher J
CJ
Livermore
David G
DG
Mordaunt
Jackie E
JE
Nerozzi
Fabrizio
F
Patel
Mamta
M
Perren
Marion J
MJ
Weingarten
Gordon G
GG
Shabbir
Shalia
S
Woollard
Patrick M
PM
Zhou
Ping
P
D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D015195:Drug Design; D005260:Female; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D051381:Rats; D018045:Receptors, Oxytocin / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship; D014590:Uterine Contraction / Q000187:drug effects
D001572:Benzofurans; D018045:Receptors, Oxytocin; D010121:Oxytocin