SYNTHESIS AND DOPAMINE ANTAGONIST ACTIVITY OF 2-THIOETHER DERIVATIVES OF THE ERGOLINE RING-SYSTEM

被引:14
作者
TUPPER, DE [1 ]
PULLAR, IA [1 ]
CLEMENS, JA [1 ]
FAIRHURST, J [1 ]
RISIUS, FC [1 ]
TIMMS, GH [1 ]
WEDLEY, S [1 ]
机构
[1] ELI LILLY & CO,LILLY RES LAB,LILLY CORP CTR,INDIANAPOLIS,IN 46285
关键词
D O I
10.1021/jm00059a017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 2-thioether derivatives of a number of clavine alkaloid (ergoline) ring systems have been synthesized and tested for dopamine antagonist activity. Of the compounds tested 2-(methylthio)-agroclavine (8,9-didehydro-6,8-dimethyl-2-(methylthio)ergoline) (6) was the most potent and had a profile of activity in animal models indicative of potential antipsychotic activity. The synthesis and biological activity of a number of metabolites of 6, including the 13-hydroxy derivative, are also reported.
引用
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页码:912 / 918
页数:7
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