N-substituted dibenzoxazepines as analgesic PGE2 antagonists.
N-substituted dibenzoxazepines as analgesic PGE2 antagonists.
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DOI：
10.1002/chin.199411197
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发表时间：
1993-10
影响因子：
7.3
通讯作者：
E. Hallinan;T. Hagen;R. K. Husa;S. Tsymbalov;S. N. Rao;J. Vanhoeck;M. Rafferty;A. Stapelfeld;M. Savage;M. Reichman
中科院分区：
文献类型：
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作者：
E. Hallinan;T. Hagen;R. K. Husa;S. Tsymbalov;S. N. Rao;J. Vanhoeck;M. Rafferty;A. Stapelfeld;M. Savage;M. Reichman
8-氯二苯[b，f][1,4]恶氮平-10(11H)-羧酸，2-乙酰肼（1,sc -19220）是一种选择性的EP1受体亚型的PGE2拮抗剂，具有抗伤性活性。SC-19220的类似物已被合成，其中乙酰基部分已被吡啶丙酰基及其同源物取代，如化合物13和29所示。这些和该系列的其他成员已被证明是有效的镇痛药和EP1亚型的PGE2拮抗剂。本报告讨论了本系列中的结构活动关系。
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.