DOPAMINE AUTORECEPTOR AGONISTS - COMPUTATIONAL STUDIES, SYNTHESIS AND BIOLOGICAL INVESTIGATIONS

被引:17
作者
GMEINER, P [1 ]
SOMMER, J [1 ]
MIERAU, J [1 ]
HOFNER, G [1 ]
机构
[1] BOEHRINGER INGELHEIM KG,BIOCHEM FORSCH ABT,W-6507 INGELHEIM,GERMANY
关键词
D O I
10.1016/S0960-894X(00)80003-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Based on molecular modeling studies on the electronic properties of dopamine and dopamine agonists the pyrazolo[1,5-a]pyridine structure has been evaluated as a catechol surrogate. The azaergoline analogue 6, including this moiety has been synthesized via 1,3-dipolar cycloaddition, anionic ring closure and electrophilic amination. The target compounds (6) exhibit DA autoreceptor agonistic activity.
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页码:1477 / 1483
页数:7
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