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
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
收藏
页码:1187 / 1190
页数:4
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