Paper Report for: Bolognesi_2009_Bioorg.Med.Chem.Lett_19_4312
Reference
Title: Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action Bolognesi ML, Bartolini M, Rosini M, Andrisano V, Melchiorre C Ref: Bioorganic & Medicinal Chemistry Lett, 19:4312, 2009 : PubMed
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.
Bolognesi ML, Bartolini M, Rosini M, Andrisano V, Melchiorre C (2009) Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action Bioorganic & Medicinal Chemistry Lett19: 4312-5
Bolognesi ML, Bartolini M, Rosini M, Andrisano V, Melchiorre C (2009) Bioorganic & Medicinal Chemistry Lett19: 4312-5