SYNTHESIS OF PYRIDYL ISOSTERES OF THIOPERAMIDE AS H3-RECEPTOR HISTAMINE-ANTAGONISTS

被引：15

作者：

GANELLIN, CR ^{[1
]}

JAYES, D ^{[1
]}

KHALAF, YS ^{[1
]}

TERTIUK, W ^{[1
]}

ARRANG, JM ^{[1
]}

DEFONTAINE, N ^{[1
]}

SCHWARTZ, JC ^{[1
]}

机构：

[1] INSERM,U109,UNITE NEUROBIOL & PHARMACOL,CTR PAUL BROCA,F-75014 PARIS,FRANCE

来源：

COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS | 1991年 / 56卷 / 11A期

关键词：

D O I：

10.1135/cccc19912448

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The synthesis and evaluation as H-3-receptor histamine antagonists is described of novel isosteric analogues of thioperamide. The compounds are designed to have fewer NH groups in order to assist brain penetration. However none of the compounds is sufficiently active as an antagonist in vitro. The 2-pyridyl analogue II has K(i) = 13-mu-mol l-1.

引用

页码：2448 / 2455

页数：8

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