Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase

被引：289

作者：

Brühlmann, C

Ooms, F

Carrupt, PA

Testa, B ^{[1
]}

Catto, M

Leonetti, F

Altomare, C

Carotti, A

机构：

[1] Univ Lausanne, Inst Chim Therapeut, BEP, CH-1015 Lausanne, Switzerland

[2] Univ Bari, Dipartimento Farmacochim, I-70125 Bari, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 19期

关键词：

D O I：

10.1021/jm010894d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A set of 17 coumarin and 2 chromone derivatives with known inhibitory activity toward monoamine oxidase (MAO) A and B were tested as acetylcholinesterase (ACNE) inhibitors. All compounds inhibited ACNE with values in the micromolar range (3-100 muM). A kinetic study showed that most compounds acted as noncompetitive ACNE inhibitors. This finding may be of interest in the context of Alzheimer's disease because recent observations suggest that MAO and ACNE inhibition might decrease beta -amyloid deposition.

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页码：3195 / 3198

页数：4

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