氨基哌啶类化合物的设计合成及其对单胺递质再摄取的抑制活性.pdf
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20 6 Vol20 No6 p. 476
2010 12 98 Ch inese Journal of M ed i inalC hem istry De 2010 Sum 98
: 1005- 0108( 20 10) 06- 0476- 08
4
1 2 2 1*
郑永勇 , 俞蕾平, 郭琳 , 李建其
( 1. , 200040; 2. , 20 1203)
: 4 ( 5HT /NA /DA)
4N , ! 1 ~ ! 9,
! 10 ~ ! 17 ; ,
17, 5
: 4; ;
: R914 : A
Design, synthesis and m onoam ine reuptake inhibitors
activities of 4am inop iperidine derivatives
1 2 2 1*
ZHENG Y ongyong , YU L eip ing , GUO L in , L I Jianqi
( 1. Shanghai Institute of Pharma eu ti al Industry, Shanghai 200040, Ch ina;
2. Shanghai Institute ofM ateria M edi a, Chinese A adem y of S ien es, Shanghai 201203, Ch ina )
Abstract: A im To design and synthesize 4am inopiperid ine derivatives m onoam ine reuptake inhibitors.
M ethods The target om pounds ! 1 - ! 9 w ere prepared by N alkylation of 4am inop iperid ine derivatives,
and om pounds ! - ! w ere obtained by redu tion of ompounds ! - ! w ith N aBH . R esu ts and
10 17 1 9 4
con c u sion Seventeen new target ompounds w ere synthesized and their stru tures w ere onfirmed by HR
1
M S and HNM R. The resu lts of prelmi inary pharm a ologi al test show ed that five of seventeen om pounds
possessed d iversem onoam ine reuptake inhibitors a tivities.
K ey w ord s: 4am inop iperid ine; monoam ine reuptake inhibitor; syn thesis
, 2~ 3
[ 2]
(M AO Is) ( TCA s), , 5
, HT /NA (
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