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Coumarins Derivatives as Dual Inhibitors of Acetylcholinesterase and Monoamine Oxidase

2001; American Chemical Society; Volume: 44; Issue: 19 Linguagem: Inglês

10.1021/jm010894d

1520-4804

Corinne Brühlmann, Frédéric Ooms, Pierre‐Alain Carrupt, Bernard Testa, Marco Catto, Francesco Leonetti, Cosimo Altomare, Angelo Carotti,

Chemical synthesis and alkaloids

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