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

Citation
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
Citations number
19
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
7
Issue
1
Year of publication
1997
Pages
1 - 6
Database
ISI
SICI code
0960-894X(1997)7:1<1:SAEOTA>2.0.ZU;2-E
Abstract
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