Donepezil: A review of the recent structural modifications and their impact on anti-Alzheimer activity

Authors

  • Noor ul Amin Mohsin Government College University Faisalabad, Faculty of Pharmaceutical Sciences, Department of Pharmaceutical Chemistry https://orcid.org/0000-0002-9366-9381
  • Matloob Ahmad Government College University Faisalabad, Department of Chemistry

DOI:

https://doi.org/10.1590/s2175-97902019000418325

Keywords:

Acetylcholinesterase (AChE), Butyrylcholinesterase (BuChE), Benzylpiperidine, Indanone, Hybrid compounds

Abstract

Alzheimer disease (AD) is characterized by a low level of acetylcholine, beta-amyloid (Aβ) aggregation and oxidative stress. Donepezil is the core medicine used for the treatment of AD. Various structural modifications of donepezil have been carried out. Benzylpiperidine part of donepezil has been replaced with benzylpyridine, pyridyl methylpiperidine, benzylpiperazine, pyrimidyl piperazine. These derived molecules showed promising activities as anti-Alzheimer agents. Replacement of indanone part by other heterocyclic rings such as pyridine resulted in the formation of compounds which exhibited monoamine oxidase (MAO) as well as acetylcholinesterase (AChE) inhibition. Propargylamine containing derivatives displayed AChE as well as MAO inhibition properties. Attachment of donepezil with natural compounds like ferulic acid, flavonoids, and curcumin showed antioxidant activities in addition to inhibition of the AChE. Benzylpiperidine and benzylpiperazine have also been combined with condensed heterocyclic rings and these compounds displayed promising anti-Alzheimer properties. This review highlights the important structural modifications of donepezil and their influence on biological activities as antiAlzheimer agents.

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Published

2020-12-09

How to Cite

Mohsin, N. ul A. ., & Ahmad, M. (2020). Donepezil: A review of the recent structural modifications and their impact on anti-Alzheimer activity. Brazilian Journal of Pharmaceutical Sciences, 56, e18325. https://doi.org/10.1590/s2175-97902019000418325

Issue

Section

Review