2. Academic Validation
  3. 3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy

3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy

  • J Med Chem. 2003 Jun 5;46(12):2279-82. doi: 10.1021/jm0340602.
Lorna Piazzi 1,  Angela Rampa,  Alessandra Bisi,  Silvia Gobbi,  Federica Belluti,  Andrea Cavalli,  Manuela Bartolini,  Vincenza Andrisano,  Piero Valenti,  Maurizio Recanatini
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, Italy.
PMID: 12773032 DOI: 10.1021/jm0340602
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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