SAR STUDIES OF FLUORINE-SUBSTITUTED BENZYLAMINES AND SUBSTITUTED 2-PHENYLETHYLAMINES AS SUBSTATES AND INACTIVATORS OF MONOAMINE-OXIDASE-B

被引：13

作者：

SILVERMAN, RB ^{[1
]}

HAWE, WP ^{[1
]}

机构：

[1] NORTHWESTERN UNIV, DEPT BIOCHEM MOLEC BIOL & CELL BIOL, EVANSTON, IL 60208 USA

来源：

JOURNAL OF ENZYME INHIBITION | 1995年 / 9卷 / 03期

关键词：

STRUCTURE-ACTIVITY RELATIONSHIPS; FLUORINATED BENZYLAMINES; SUBSTITUTED; 2-PHENYLETHYLAMINES; MONOAMINE OXIDASE B;

D O I：

10.3109/14756369509021486

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

To test whether addition of electron-withdrawing substituents to good substrates of monoamine oxidase (MAO) will transform them into inactivators, a series of fluorine-substituted benzylamines and a series of substituted 2-phenylethylamines were synthesized and tested as substrates and inactivators of monoamine oxidase B. All of the compounds were substrates. None of the benzylamines was an inactivator, but several of the phenethylamines were. These results suggest that either stronger electron withdrawing character or additional stabilizing factors are needed to stabilize the hypothesized enzyme adduct.

引用

页码：203 / 215

页数：13

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