SUBSTITUTED XANTHONES AS SELECTIVE AND REVERSIBLE MONOAMINE OXIDASE-A (MAO-A) INHIBITORS

被引：37

作者：

THULL, U

KNEUBUHLER, S

TESTA, B

BORGES, MFM

PINTO, MMM

机构：

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

[2] FAC FARM PORTO, QUIM ORGAN LAB, P-4000 OPORTO, PORTUGAL

来源：

PHARMACEUTICAL RESEARCH | 1993年 / 10卷 / 08期

关键词：

DIHYDROXYMETHYLXANTHONES; MONOAMINE OXIDASE (MAO); MAO-A; SELECTIVE REVERSIBLE INHIBITORS;

D O I：

10.1023/A:1018924503552

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

1,3-Dihydroxy-2-methylxanthone (X1), its 4-chloro and 4-bromo derivatives (X1-Cl and X1-Br), and 1,3-dihydroxy-4-methylxanthone were investigated for their inhibition activities toward MAO. A hyperbolic function was derived to fit the data and to calculate IC50 values. The compounds proved to be reversible and selective inhibitors of MAO-A, with X1 displaying the highest activity (IC50 = 3.7 muM).

引用

页码：1187 / 1190

页数：4

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