具有顺式双环[4.3.0]壬烯环系的化学稳定前列环素类似物的合成与生物活性：新型高异卡前列素类似物

Syntheses and biological activities of chemically stable prostacyclin mimics with cis-bicyclo[4.3.0]nonene ring system: the novel homoisocarbacyclin analogues.

作者信息

Narita S, Takahashi A, Aoki T, Sato H, Satoh S, Yamada S, Kudo M, Yamaguchi T, Kogi K, Shibasaki M

机构信息

Fukushima Research Laboratories, TOA EIYO Ltd., Japan.

出版信息

Bioorg Med Chem. 1993 Aug;1(2):77-118. doi: 10.1016/s0968-0896(00)82108-2.

DOI:10.1016/s0968-0896(00)82108-2

PMID:8081847

Abstract

The synthetic studies concerning a series of homoisocarbacyclin analogues, which are homologous compounds of isocarbacyclin, with cis-bicyclo[4.3.0]non-2-ene or cis-bicyclo[4.3.0]non-3-ene as a nucleus have been carried out. The general synthetic methods of homoisocarbacyclin analogues have been accomplished starting with the versatile Corey lactone. Among the analogues synthesized in the present studies, a promising compound (TY-11223) exhibiting a good selectivity in biological actions was found to be studied further.

摘要

已经开展了一系列高异卡前列素类似物的合成研究，这些类似物是以异卡前列素为同源化合物，以顺式双环[4.3.0]壬-2-烯或顺式双环[4.3.0]壬-3-烯为核心。高异卡前列素类似物的一般合成方法已从通用的科里内酯开始得以实现。在本研究中合成的类似物中，发现了一种在生物活性方面表现出良好选择性的有前景的化合物（TY-11223），有待进一步研究。