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
引用
收藏
页码:1 / 6
页数:6
相关论文
共 19 条
[1]  
BUTZ RF, 1982, J PHARMACOL EXP THER, V221, P676
[2]  
KENT RE, 1955, ORG SYNTH, V4, P490
[3]  
Kharasch M.S., 1954, GRIGNARD REACTIONS N, P767
[4]  
KOSHINAKA E, 1979, CHEM ABSTR 132710, V90
[5]  
Krynitsky JA, 1963, ORG SYNTH, VIV, P436
[6]   EFFECT OF DESMETHYLIMIPRAMINE, IPRINDOLE AND DL-ERYTHRO-ALPHA-(3,4-DICHLOROPHENYL)-BETA-(TERT-BUTYL AMINO) PROPANOL HCL ON METABOLISM OF AMPHETAMINE [J].
LEMBERGER, L ;
SERNATINGER, E ;
KUNTZMAN, R .
BIOCHEMICAL PHARMACOLOGY, 1970, 19 (12) :3021-+
[7]  
Mehta N. B., 1974, US Pat, Patent No. 3819706
[8]   DESIGN AND SYNTHESIS OF A HAPTEN FOR THE RADIOIMMUNOASSAY OF BUPROPION [J].
MEHTA, NB ;
MUSSO, DL .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1986, 75 (04) :410-412
[9]   POTENTIAL ANTICONVULSANTS .1. 5-BENZYLHYDANTOINS [J].
MEHTA, NB ;
DIUGUID, CAR ;
SOROKO, FE .
JOURNAL OF MEDICINAL CHEMISTRY, 1981, 24 (04) :465-468
[10]  
MUELLER HK, 1971, J PRAKT CHEM, V313, P1