结构活性研究导向一种组织选择性降压前列腺素类似物，13,14-二氢-16-苯基-ω-四降前列环素E2。

Structure activity studies leading to a tissue-selective hypotensive prostaglandin analog, 13,14-dihydro-16-phenyl-omega-tetranor PGE2.

作者信息

Johnson M R, Schaaf T K, Constantine J W, Hess H J

出版信息

Prostaglandins. 1980 Sep;20(3):515-20. doi: 10.1016/0090-6980(80)90039-8.

Abstract

During our systematic search for prostaglandins with improved tissue selectivity and metabolic stability, we synthesized a series of PGE2 analogs in which the n-amyl carbinol side chain was systematically substituted by a phenyl ring, based on structural considerations incorporating the 17,18-cis-double bond of PGE1 into an aromatic ring. These compounds were evaluated for uterine stimulant, bronchodilator and hypotensive activity. Among the divergent biological profiles exhibited by these analogs, noteworthy was the tissue-selective hypotensive profile displayed by 13,14-dihydro-16-phenyl-omega-tetranor PGE2.

摘要

在我们对具有改善的组织选择性和代谢稳定性的前列腺素进行系统研究的过程中，基于将PGE1的17,18-顺式双键并入芳香环的结构考虑，我们合成了一系列PGE2类似物，其中正戊基甲醇侧链被苯环系统取代。对这些化合物的子宫兴奋、支气管扩张和降压活性进行了评估。在这些类似物所呈现的不同生物学特性中，值得注意的是13,14-二氢-16-苯基-ω-四降PGE2所表现出的组织选择性降压特性。