| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10596422 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
The present article expands on the study of structure-activity relationships of the novel class of quinone-bearing polyamines, as multi-target-directed ligands against Alzheimer's disease. Namely, the effect of inserting a methyl substituent at the α position of the terminal benzyl amine moieties of lead candidate 1 (memoquin) was evaluated at the multiple targets involved in the multifunctional mechanism of action. The RR stereoisomer 2 resulted more effective than 1 in reverting two important effects mediated by acetylcholinesterase (AChE), that is, acetylcholine hydrolysis and AChE-induced amyloid-β aggregation.
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Authors
Maria Laura Bolognesi, Manuela Bartolini, Michela Rosini, Vincenza Andrisano, Carlo Melchiorre,