Synthesis and Dopamine Antagonist Activity of 2-Thioether Derivatives of the Ergoline Ring System

Article abstract of DOI:10.1021/jm00059a017

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.