9,11-偶氮-13-氧杂-15-羟基前列腺烷酸（一种强效血小板聚集抑制剂）的合成与生物学评价

Synthesis and biological evaluation of 9,11-azo-13-oxa-15-hydroxyprostanoic acid, a potent inhibitor of platelet aggregation.

作者信息

Kam S T, Portoghese P S, Gerrard J M, Dunham E W

出版信息

J Med Chem. 1979 Nov;22(11):1402-8. doi: 10.1021/jm00197a023.

Abstract

The synthesis of a prostaglandin endoperoxide analogue, 9,11-azo-13-oxa-15-hydroxyprostanoic acid (AOHP), is described. AOHP was found to block effectively both the thromboxane synthetase and the PGH2/TxA2 receptors in human platelets. It inhibits the platelet aggregation induced by arachidonic acid, 9.11-methanoepoxy-PGH2, PGH2, and TxA2 but does not affect the ADP-induced aggregation in aspirinated platelet-rich plasma. Some of the intermediates for the synthesis of AOHP also are effective in inhibiting platelet aggregation.

摘要

本文描述了一种前列腺素内过氧化物类似物9,11-偶氮-13-氧杂-15-羟基前列腺酸（AOHP）的合成。研究发现，AOHP能有效阻断人血小板中的血栓素合成酶和PGH2/TxA2受体。它可抑制花生四烯酸、9,11-亚甲基环氧-PGH2、PGH2和TxA2诱导的血小板聚集，但不影响富血小板血浆中阿司匹林处理后的ADP诱导的聚集。AOHP合成过程中的一些中间体在抑制血小板聚集方面也有效。