4.7 Article

Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase

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JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 19, 页码 3195-3198

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AMER CHEMICAL SOC
DOI: 10.1021/jm010894d

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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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