SCREENING OF UNSUBSTITUTED CYCLIC-COMPOUNDS AS INHIBITORS OF MONOAMINE OXIDASES

被引：86

作者：

THULL, U ^{[1
]}

TESTA, B ^{[1
]}

机构：

[1] UNIV LAUSANNE, ECOLE PHARM, INST CHIM THERAPEUT, CH-1015 LAUSANNE, SWITZERLAND

来源：

BIOCHEMICAL PHARMACOLOGY | 1994年 / 47卷 / 12期

关键词：

MONOAMINE OXIDASES (MAO); UNSUBSTITUTED ARENES; UNSUBSTITUTED AZAHETEROCYCLES; UNSUBSTITUTED OXAHETEROCYCLES; XANTHONE;

D O I：

10.1016/0006-2952(94)90271-2

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A number of unsubstituted aromatic hydrocarbons, azaheterocycles, oxaheterocycles and cyclic ketones were screened for their inhibitory potency towards monoamine oxidases (MAO; EC 1.4.3.4.) A and B. Fair activities (IC50 10-100 mu M) and selectivities were found for, e.g. naphthalene, anthracene, phenanthrene, isoquinoline and acridine. The most active inhibitors are oxygen-containing compounds (e.g. coumarin, flavone, dibenzofuran, xanthene, thioxanthone and acridone), with xanthone emerging as a potent (IC50 0.8 mu M) and reversible MAO-A inhibitor. All tested inhibitors seem to act in a reversible and time-independent manner.

引用

页码：2307 / 2310

页数：4

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