Literature

Abstract

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.

DOI： 10.1021/acsmedchemlett.5b00483

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

ACS Medicinal Chemistry Letters 2016.0

Structure-based design, synthesis, and evaluation of structurally rigid donepezil analogues as dual AChE and BACE-1 inhibitors

Bioorganic & Medicinal Chemistry Letters 2018.0

Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer’s disease

Bioorganic & Medicinal Chemistry Letters 2015.0

Design, synthesis and biological activity of novel donepezil derivatives bearing N -benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors

European Journal of Medicinal Chemistry 2017.0

Design, synthesis and biological evaluation of novel donepezil–coumarin hybrids as multi-target agents for the treatment of Alzheimer’s disease

Bioorganic & Medicinal Chemistry 2016.0

Novel Donepezil-Based Inhibitors of Acetyl- and Butyrylcholinesterase and Acetylcholinesterase-Induced β-Amyloid Aggregation