Structure−Activity Relationships of Acetylcholinesterase Noncovalent Inhibitors Based on a Polyamine Backbone. 4. Further Investigation on the Inner Spacer

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• 作者：Vincenzo Tumiatti ; Andrea Milelli ; Anna Minarini ; Michela Rosini ; Maria Laura Bolognesi ; Marialuisa Micco ; Vincenza Andrisano ; Manuela Bartolini ; Francesca Mancini ; Maurizio Recanatini ; Andrea Cavalli
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：November 27, 2008
• 年：2008
• 卷：51
• 期：22
• 页码：7308-7312
• 全文大小：166K
• 年卷期：v.51,no.22(November 27, 2008)
• ISSN：1520-4804

文摘

Novel multi-target-directed ligands were designed by replacing the inner dipiperidino function of 3 with less flexible or completely rigid moieties to obtain compounds endowed with multiple biological properties that might be relevant to Alzheimer’s disease. 15 was the most interesting, inhibiting AChE in the nanomolar range and inhibiting AChE-induced and self-promoted β-amyloid aggregation in the micromolar range.