## Abstract The lipophilicity of a number of __N__โacyl derivatives of __trans__โ or __cis__โ: racemic, (1__R__,2__R__)โ or (1__S__,2__S__)โaminocyclohexanol (1โ13) exhibiting anticonvulsant activity was investigated. Their lipophilicity (__R__~m0~) was determined using reversedโphase thinโlayer ch
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
โ Scribed by David L. Musso; Nariman B. Mehta; Francis E. Soroko
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- English
- Weight
- 229 KB
- Volume
- 7
- Category
- Article
- ISSN
- 0960-894X
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โฆ Synopsis
A series of 2-amino-l-phenyl-l-propanols that are structurally related to known metabolites of bupropion,1 (Wellbutrinยฎ) were synthesized and evaluated as potential anticonvulsants. The (R*,R*)-2tert-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.
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