N-Substituted Dibenzoxazepines as Analgesic PGE2 Antagonists

Article abstract of DOI:10.1021/jm00074a010

8-Chlorodibenz<1,4>oxazepine-10(11H)-carboxylic acid, 2-acetylhydrazide (1, SC-19220) has been previously reported by us and others to be a PGE₂ antagonist selective for the EP₁ receptor subtype with antinociceptive activities.Analogs of SC-19220, in which the acetyl moiety has been replaced with pyridylpropionyl groups and their homologs, have been synthesized as illustrated by compounds 13 and 29.These and other members of this series have been shown to be efficacious analgesics and PGE₂ antagonists of the EP₁ subtype.This report discusses the structure activity relationships within this series.