Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors

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• 作者：Paola Costanzo ; Luca Cariati ; Doriana Desiderio ; Roberta Sgammato ; Anna Lamberti ; Rosaria Arcone ; Raffaele Salerno ; Monica Nardi ; Mariorosario Masullo ; Manuela Oliverio
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：May 12, 2016
• 年：2016
• 卷：7
• 期：5
• 页码：470-475
• 全文大小：382K
• 年卷期：0
• ISSN：1948-5875

文摘

An ecofriendly synthetic pathway for the synthesis of donepezil precursors is described. Alternative energy sources were used for the total synthesis in order to improve yields, regioselectively, and rate of each synthetic step and to reduce the coproduction of waste at the same time. For all products, characterized by an improved structural rigidity respect to donepezil, the inhibitor activity on AChE, the selectivity vs BuChE, the side-activity on BACE-1, and the effect on SHSY-5Y neuroblastoma cells viability were tested. Two potential new lead compounds for a dual therapeutic strategy against Alzheimer’s disease were envisaged.