初级前列腺素13-脱氢衍生物的合成与药理活性

Synthesis and pharmacological activities of 13-dehydro derivatives of primary prostaglandins.

作者信息

Tanami T, Kameo K, Ono N, Nakagawa T, Annou S, Tsuboi M, Tani K, Okamoto S, Sato F

机构信息

Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.

出版信息

Bioorg Med Chem Lett. 1998 Jun 16;8(12):1507-10. doi: 10.1016/s0960-894x(98)00247-9.

DOI:10.1016/s0960-894x(98)00247-9

PMID:9873379

Abstract

13-Dehydro derivatives of prostaglandin E1, E2, E3, F1 alpha and F2 alpha were synthesized. Compared with natural prostaglandins, 13-dehydro analogues were found to exhibit more potent inhibitory activity against human platelet aggregation and relaxation of guinea-pig isolated trachea, while they showed less potent activity of contraction of guinea-pig isolated ileum.

摘要

合成了前列腺素E1、E2、E3、F1α和F2α的13 - 脱氢衍生物。与天然前列腺素相比，发现13 - 脱氢类似物对人血小板聚集和豚鼠离体气管舒张表现出更强的抑制活性，而对豚鼠离体回肠收缩的活性则较弱。