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• W2059163911 abstract "Memoquin (1) is a lead compound multitargeted against Alzheimer's disease (AD). It is an AChE inhibitor, free-radical scavenger, and inhibitor of amyloid-β (Aβ) aggregation. A new series of 1 derivatives was designed and synthesized by linking its 2,5-diamino-benzoquinone core with motifs that are present in the structure of known amyloid binding agents like curcumin, the benzofuran derivative SKF64346, or the benzothiazole bearing compounds KHG21834 and BTA-1. The weaker AChE inhibitory potencies and the concomitant nearly equipotent anti-amyloid activities of the new compounds with respect to 1 resulted in a more balanced biological profile against both targets. Selected compounds turned out to be effective Aβ aggregation inhibitors in a cell-based assay. By properly combining two or more distinct pharmacological properties in a molecule, we can achieve greater effectiveness compared to single-targeted drugs for investigating AD." @default.
• W2059163911 created "2016-06-24" @default.
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• W2059163911 date "2011-05-01" @default.
• W2059163911 modified "2023-10-12" @default.
• W2059163911 title "Multitargeted drugs discovery: Balancing anti-amyloid and anticholinesterase capacity in a single chemical entity" @default.
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• W2059163911 doi "https://doi.org/10.1016/j.bmcl.2010.12.093" @default.
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