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Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase

Bruhlmann, C.
Ooms, F.
Testa, Bernard
Catto, M.
Leonetti, F.
Altomare, Cosimo
Carotti, Angelo
Published in Journal of medicinal chemistry. 2001, vol. 44, no. 19, p. 3195-3198
Abstract 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.
Keywords Acetylcholinesterase/chemistryAnimalsCholinesterase Inhibitors/*chemical synthesis/chemistryCoumarins/*chemical synthesis/chemistryEelsMonoamine Oxidase Inhibitors/*chemical synthesis/chemistryStructure-Activity Relationship
PMID: 11543689
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BRUHLMANN, C. et al. Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase. In: Journal of medicinal chemistry, 2001, vol. 44, n° 19, p. 3195-3198. doi: 10.1021/jm010894d

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Deposited on : 2010-08-06

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