3-(4-{[Benzyl(methyl)amino]methyl}phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) Inhibits Both Acetylcholinesterase and Acetylcholinesterase-Induced β-Amyloid Aggregation: A Dual Function Lead for Alzheimer's Disease Therapy
Journal of Medicinal Chemistry2003Vol. 46(12), pp. 2279–2282
Citations Over TimeTop 10% of 2003 papers
Lorna Piazzi, Angela Rampa, Alessandra Bisi, Silvia Gobbi, Federica Belluti, Andrea Cavalli, Manuela Bartolini, Vincenza Andrisano, Piero Valenti, Maurizio Recanatini
Abstract
In recent years, the investigation of acetylcholinesterase (AChE) inhibitors has gained further interest, because the involvement of the peripheral site of the enzyme in the beta-amyloid (Abeta) aggregation process has been disclosed. We present here, for the first time, a direct evidence of the Abeta antiaggregating action of an AChE inhibitor (AP2238) purposely designed to bind at both the catalytic and the peripheral sites of the human enzyme.
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