SYNTHESIS OF DL-CIS- AND (4R,5R)-TRANS-7-[2,2-DIMETHYL-4-(PHENYLSULFONYL)-AMINOMETHYL-1,3-DIOXOLAN-5-YL]-5(Z)-HEPTENOIC ACID ANALOGS AS PLATELET THROMBOXANE A(2) RECEPTOR ANTAGONISTS

被引：9

作者：

KOMIOTIS, D

PANANOOKOOLN, S

ZAW, K

DIETER, JP

LEBRETON, GC

VENTON, DL

机构：

[1] UNIV ILLINOIS, DEPT MED CHEM & PHARMACOGNOSY, CHICAGO, IL 60680 USA

[2] UNIV ILLINOIS, DEPT PHARMACOL, CHICAGO, IL 60612 USA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 30卷 / 04期

基金：

美国国家卫生研究院;

关键词：

THROMBOXANE A(2); RECEPTOR ANTAGONIST; PLATELET AGGREGATION; 1,3-DIOXOLANE;

D O I：

10.1016/0223-5234(96)88240-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The title compounds have been synthesized and their in vitro thromboxane A(2) (TxA(2)) receptor antagonist activity evaluated. Both cis and trans isomers (1, 2) were shown to specifically inhibit submaximal human platelet aggregation induced by 225 nM U46619 in a dose-dependent manner with an IC50 of 1 mu M. The concentration of 1 and 2 required to completely block maximal aggregation induced by 3 mu M U46619 was 3 mu(M).

引用

页码：321 / 326

页数：6

共 24 条

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BORN GVR, 1963, J PHYSIOL-LONDON, V168, P178, DOI 10.1113/jphysiol.1963.sp007185

[2] THE SYNTHESIS OF A NOVEL THROMBOXANE RECEPTOR ANTAGONIST 4(Z)-6-(2-O-CHLOROPHENYL-4-O-HYDROXYPHENYL-1,3-DIOXAN-CIS-5-YL) HEXENOIC ACID ICI 192605 [J].