INHIBITORS OF MONOAMINE OXIDASE .3. 9-SUBSTITUTED-BETA-CARBOLINES

被引:19
作者
HO, BT
MCISAAC, WM
TANSEY, LW
WALKER, KE
机构
[1] Biological Research Division, Texas Research Institute of Mental Sciences, Houston, Texas
关键词
IR spectrophotometry—structure; Monoamine oxidase (MAO) inhibitors—synthesis; Pharmacological screening—β‐carbolines; MAO inhibitors; UV spectrophotometry—structure; β‐Carbolines; 9‐substituted—synthesis;
D O I
10.1002/jps.2600580217
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 9‐alkyl aromatic‐β‐carbolines was synthesized and evaluated as inhibitors of mitrochondrial monoamine oxidase. The possible existence of a hydrophobic or hydrophilic region on the enzyme was explored. Substitution of an electron‐withdrawing group such as acetyl on N‐9 position reduced the inhibitory activity. This suggested that the increase in the inhibitory activity of 9‐methyl‐β‐carboline was at least partially due to the increase of its electron density by the methyl group, thus making the β‐carboline bind better to the enzyme. Copyright © 1969 Wiley‐Liss, Inc., A Wiley Company
引用
收藏
页码:219 / &
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