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

DL Musso, NB Mehta, FE Soroko

Index: Musso, David L.; Mehta, Nariman B.; Soroko, Francis E. Bioorganic and Medicinal Chemistry Letters, 1997 ,  vol. 7,  # 1  p. 1 - 6

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Citation Number: 20

Abstract

A series of 2-amino-1-phenyl-1-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-1-(3-trifluoromethylphenyl) propanol 20 had an ED50 of 16.5±2.8 mg/kg ip in mice in the maximal electroshock screen and was chosen for further evaluation.