Journal of Medicinal Chemistry p. 912 - 918 (1993)
Update date:2022-08-17
Topics:
Tupper, David E.
Pullar, Ian A.
Clemens, James A.
Fairhurst, John
Risius, Francesca C.
et al.
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.
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