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 et al., 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, 7(1), 1997, pp. 1-6
A series of 2-amino-1-phenyl-1-propanols that are structurally related
to known metabolites of bupropion,1 (Wellbutrin(R)) were synthesized
and evaluated as potential anticonvulsants. The ,R)-2-tert-butylamino
-1-(3-trifluoromethylphenyl) propanol 20 had an ED(50) of 16.5 +/- 2.8
mg/kg ip in mice in the maximal electroshock screen and was chosen fo
r further evaluation. Copyright (C) 1996 Elsevier Science Ltd