Inhibition of Acetylcholinesterase, β-Amyloid Aggregation, and NMDA Receptors in Alzheimer’s Disease: A Promising Direction for the Multi-target-Directed Ligands Gold Rush

Alzheimer’s disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. To confront AD, an innovative strategy is to design single chemical entities able to simultaneously modulate more than one target. Here, we present compounds that inhibit acetylcholineste...

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Veröffentlicht in:Journal of medicinal chemistry 2008-08, Vol.51 (15), p.4381-4384
Hauptverfasser: Rosini, Michela, Simoni, Elena, Bartolini, Manuela, Cavalli, Andrea, Ceccarini, Luisa, Pascu, Nicoleta, McClymont, David W, Tarozzi, Andrea, Bolognesi, Maria L, Minarini, Anna, Tumiatti, Vincenzo, Andrisano, Vincenza, Mellor, Ian R, Melchiorre, Carlo
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Sprache:eng
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Zusammenfassung:Alzheimer’s disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. To confront AD, an innovative strategy is to design single chemical entities able to simultaneously modulate more than one target. Here, we present compounds that inhibit acetylcholinesterase and NMDA receptor activity. Furthermore, these compounds inhibit AChE-induced Aβ aggregation and display antioxidant properties, emerging as lead candidates for treating AD.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm800577j