Coumarins Derivatives as Dual Inhibitors of Acetylcholinesterase and Monoamine Oxidase 论文

2001Journal of Medicinal Chemistry引用 289
Cholinesterase and Neurodegenerative DiseasesComputational Drug Discovery MethodsChemical synthesis and alkaloids

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 (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.