Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.
Structure-activity studies on the oxytocin antagonist 1 (L-371,257) have identified a new series of high affinity, receptor-selective OT antagonists in which the N-acetyl-4-piperidinyl ether terminus in 1 has been replaced with a 1-(aryl)ethoxy group.
Kuo
M S
MS
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
Bock
M G
MG
Freidinger
R M
RM
Guidotti
M T
MT
Lis
E V
EV
Pawluczyk
J M
JM
Perlow
D S
DS
Pettibone
D J
DJ
Quigley
A G
AG
Reiss
D R
DR
Williams
P D
PD
Woyden
C J
CJ
D000284:Administration, Oral; D000818:Animals; D048588:Benzoxazines; D001682:Biological Availability; D005260:Female; D006801:Humans; D010078:Oxazines / Q000494:pharmacology*; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D048588:Benzoxazines; C096766:L 371257; D010078:Oxazines; D010880:Piperidines; D010121:Oxytocin