HYDROXYINDOLE-O-METHYLTRANSFERASE .3. INFLUENCE OF PHENYL MOIETY ON INHIBITORY ACTIVITIES OF SOME N-ACYLTRYPTAMINES

被引：17

作者：

HO, BT

MCISAAC, WM

TANSEY, LW

机构：

[1] Biological Research Division, Texas Research Institute of Mental Sciences, Houston, Texas

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1969年 / 58卷 / 05期

关键词：

Hydroxyindole‐O‐methyltransferase inhibition—N‐acyltryptamines; IR spectrophotometry—identity; structure; N‐Acyltryptamines—synthesis; Structureactivity relationship—N‐acyltryptamines; UV spectrophotometry—identity;

D O I：

10.1002/jps.2600580508

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

During previous studies on the inhibition of hydroxyindole‐O‐methyltransferase, several N‐acyltryptamines have been found to be good inhibitors of this enzyme. Substitution of the benzyl or phenyl moiety of N‐phenylacetyltryptamine or N‐benzoyltryptamine with halogen atoms further enhanced the inhibitory activity. Among all the halogen‐substituted inhibitors, the 3,4‐dichloro substitution offered the highest activity. An increase in inhibition of the enzyme was also observed when a fluorine or bromine atom was placed on C‐5 position of the indole nucleus. A combination of the 5‐bromo and 3,4‐dichlorobenzoyl substitutions resulted in the most active inhibitor. Copyright © 1969 Wiley‐Liss, Inc., A Wiley Company

引用

页码：563 / &

共 8 条

[1]

AXELROD J, 1961, J BIOL CHEM, V236, P211

[2]

ANALOGS OF TETRAHYDROFOLIC ACID .29. HYDROPHOBIC BONDING TO DIHYDROFOLIC REDUCTASE .2. ON MODE OF PHENYL BINDING OF 1-ARYL-4,6-DIAMINO-1,2-DIHYDRO-2,2-DIMETHYL-S-TRIAZINES [J].