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

被引:16
作者
Musso, DL
Mehta, NB
Soroko, FE
机构
[1] BURROUGHS WELLCOME CO,DIV ORGAN CHEM,RES TRIANGLE PK,NC 27709
[2] BURROUGHS WELLCOME CO,DIV PHARMACOL,RES TRIANGLE PK,NC 27709
关键词
D O I
10.1016/S0960-894X(96)00577-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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*,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 for further evaluation. Copyright (C) 1996 Elsevier Science Ltd
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页码:1 / 6
页数:6
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