Literature

Abstract

Amyloid beta (Aβ) and cholinesterase enzymes (AChE, BuChE) are important biological targets for the effective treatment of Alzheimer's disease. In this study, the aim was to synthesize new donepezil-like secondary amide compounds that display a potent inhibition of cholinesterases and Aβ with antioxidant and metal chelation abilities. All test compounds showed activities against both ChEs and β1-42 inhibition. The most encouraging compound, 20, is an AChE inhibitor with high anti-aggregation activity (55.3%). Based on the results, compound 20 may be a promising structure in further research for new anti-Alzheimer's agents.

DOI： 10.1016/j.bmcl.2015.10.051

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

Bioorganic & Medicinal Chemistry Letters 2015.0

Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo

Bioorganic & Medicinal Chemistry 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

Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation

European Journal of Medicinal Chemistry 2016.0

Isoindoline-1,3-dione derivatives targeting cholinesterases: Design, synthesis and biological evaluation of potential anti-Alzheimer’s agents

Bioorganic & Medicinal Chemistry 2015.0

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