Synthesis and evaluation of the anticonvulsant activity of a series of 2-amino-1-phenyl-1-propanols derived from the metabolites of the antidepressant bupropion

Bioorganic & Medicinal Chemistry Letters
1997.0

Abstract

A series of 2-amino-l-phenyl-l-propanols that are structurally related to known metabolites of bupropion,1 (Wellbutrin®) were synthesized and evaluated as potential anticonvulsants. The (R*,R*)-2 tert-butylamino-l-(3-trifluoromethylphenyl) propanol 20 had an EDs0 of 16.5 + 2.8 mg/kg ip in mice in the maximal electroshock screen and was chosen for further evaluation. Copyright © 1996 Elsevier Science Ltd

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