Abstract
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.
MeSH terms
-
Animals
-
Benzofurans / chemical synthesis*
-
Benzofurans / pharmacokinetics
-
Benzofurans / pharmacology
-
Drug Design
-
Female
-
Humans
-
Kinetics
-
Models, Molecular
-
Molecular Conformation
-
Oxytocin / antagonists & inhibitors*
-
Rats
-
Receptors, Oxytocin / antagonists & inhibitors
-
Receptors, Oxytocin / metabolism
-
Structure-Activity Relationship
-
Uterine Contraction / drug effects
Substances
-
Benzofurans
-
Receptors, Oxytocin
-
Oxytocin