Hallinan E A, Hagen T J, Husa R K, Tsymbalov S, Rao S N, vanHoeck J P, Rafferty M F, Stapelfeld A, Savage M A, Reichman M
Department of Chemical Research, Searle, Skokie, Illinois 60077.
J Med Chem. 1993 Oct 29;36(22):3293-9. doi: 10.1021/jm00074a010.
8-Chlorodibenz[b,f][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.
8-氯二苯并[b,f][1,4]恶氮杂卓-10(11H)-羧酸2-乙酰肼（1，SC-19220），我们和其他人之前已报道其为对EP1受体亚型具有选择性的PGE2拮抗剂，具有抗伤害感受活性。已合成SC-19220的类似物，其中乙酰基部分已被吡啶基丙酰基及其同系物取代，如化合物13和29所示。该系列的这些及其他成员已被证明是有效的镇痛药和EP1亚型的PGE2拮抗剂。本报告讨论了该系列内的构效关系。
