Structure-activity relationships of substituted 5H-thiazolo [3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists

被引：90

作者：

Wichmann, J ^{[1
]}

Adam, G ^{[1
]}

Kolczewski, S ^{[1
]}

Mutel, V ^{[1
]}

Woltering, T ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Div Pharma, Preclin CNS Res, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(99)00227-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5H-thiazolo[3,2-a]pyrimidine derivatives 1 was studied with respect to the inhibition of 1S,3R-ACPD (10 mu M)-stimulated GTP gamma(35)S binding on rat mGlu2 receptor transfected cell membranes. The influence of substituents at position 6 and 7 as well as the substitution pattern of the two phenyl-rings in position 2 and 5 on the activity is discussed. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1573 / 1576

页数：4

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