(E)-1-(heterocyclyl or cyclohexyl)-2-[1,3,7-trisubstituted(xantkin-8-yl)] ethenes as A(2a) adenosine receptor antagonists

被引：20

作者：

DelGiudice, MR ^{[1
]}

Borioni, A ^{[1
]}

Mustazza, C ^{[1
]}

Gatta, F ^{[1
]}

Dionisotti, S ^{[1
]}

Zocchi, C ^{[1
]}

Ongini, E ^{[1
]}

机构：

[1] SCHERING PLOUGH CORP,LAB RIC,MILAN,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 31卷 / 01期

关键词：

8-styrylxanthine analogue; adenosine A(2a); receptor antagonist;

D O I：

10.1016/S0223-5234(96)80007-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Some 1,3,7-trisubstituted-8-styrylxanthine analogues, with the aryl group replaced by a heterocycle or cyclohexane ring, were prepared and evaluated for their interaction with the A(1) and A(2a) adenosine receptors. The highest degree of activity was displayed by the 1,3-dipropyl-7-methyl-8-[2-(3-thienyl)ethenyl]xanthine 4cdi, which was found to be a potent and selective A(2a) antagonist in binding assays (K-i = 19 nM, A(1)/A(2a) ratio = 30).

引用

收藏

页码：59 / 63

页数：5

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