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ID: ALA1152360
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action.
Authors: Bolognesi ML, Bartolini M, Rosini M, Andrisano V, Melchiorre C.
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.
CiteXplore: 19505825