Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists

被引:23
作者
Kolczewski, S [1 ]
Adam, G [1 ]
Stadler, H [1 ]
Mutel, V [1 ]
Wichmann, J [1 ]
Woltering, T [1 ]
机构
[1] F Hoffmann La Roche & Co Ltd, Preclin CNS Res, Div Pharma, CH-4070 Basel, Switzerland
关键词
D O I
10.1016/S0960-894X(99)00346-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Heterocyclic enol ethers of type 1 were studied with respect to the inhibition of 1S,3R-ACPD (10 mu M)stimulated GTP gamma(35)S binding on rat mGluR2 transfected cell membranes. The structure activity relationship with regard to the substitution pattern of the phenyl ring, the oxygen substituent and the nature of the heterocycle is discussed, (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2173 / 2176
页数:4
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