Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system
- 1 April 1993
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 36 (7) , 912-918
- https://doi.org/10.1021/jm00059a017
Abstract
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.Keywords
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