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EnglishThe 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 alpha 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-beta aggregation.
| Titolo: | Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action |
| Autore/i: | BOLOGNESI, MARIA LAURA; BARTOLINI, MANUELA; ROSINI, MICHELA; ANDRISANO, VINCENZA; MELCHIORRE, CARLO |
| Autore/i Unibo: | |
| Anno: | 2009 |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.bmcl.2009.05.087 |
| 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 alpha 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-beta aggregation. |
| Data prodotto definitivo in UGOV: | 2010-02-16 12:59:11 |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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