Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase
Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase
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DOI：
10.1021/jm010894d
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发表时间：
2001-09-13
影响因子：
7.3
通讯作者：
Carotti, A
中科院分区：
文献类型：
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作者：
Brühlmann, C;Ooms, F;Carotti, A
一组 17 种香豆素和 2 种色酮衍生物对单胺氧化酶 (MAO) A 和 B 具有已知的抑制活性，作为乙酰胆碱酯酶 (ACNE) 抑制剂进行了测试。所有化合物均以微摩尔范围（3-100 μM）抑制 ACNE。动力学研究表明，大多数化合物都充当非竞争性 ACNE 抑制剂。这一发现在阿尔茨海默病的背景下可能会引起人们的兴趣，因为最近的观察表明 MAO 和 ACNE 抑制可能会减少 β-淀粉样蛋白沉积。
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.