Alzheimer's disease (AD) is a progressive neurodegenerative disease with no clinically accepted treatment to cure or halt its progression. The Food and Drug Administration has approved drugs (e.g., rivastigmine, donepezil, galantamine, and memantine) that at best provide marginal benefits, thus emphasizing the urgent need to explore other molecular entities as future drug candidates for AD. Looking at the wide pharmaceutical applications of heterocyclic compounds and particularly those containing benzofuran and indole ring systems, these molecular frameworks have drawn special attention from medicinal chemists for further evaluation in numerous diseases. This article focuses on the history and recent advances of benzofuran- and indole-based compounds as inhibitors of butyrylcholinesterase, acetylcholinesterase, γ-secretase, β-secretase, tau misfolding, and β-amyloid aggregation.

https://onlinelibrary.wiley.com/doi/pdf/10.1002/cmdc.201800156

Benzofuran and Indole: Promising Scaffolds for Drug Development in Alzheimer's Disease.

Synthesis, structure–activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors

3-(Benzofuran-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde was used, as a precursor for the synthesis of a series of novel heterocycles by facile reactions with 3-oxo-3-phenylpropanenitrile, 2-cyanoethanethioamide, and various hydrazides such as cyanoacetohydrazide, acetohydrazide, and carbohydrazide derivatives. The structures of the products were confirmed by various spectroscopic methods along with the X-ray crystal structures.

A simple procedure for the synthesis of novel 3-(benzofur-2-yl)pyrazole-based heterocycles

A simple and convenient one-pot three-component method to synthesize 1,2,3-triazole-based 2,3-dihydrofuran derivatives from the condensation of 5,5-dimethylcyclohexane-1,3-dione, substituted phenacyl bromide, triethylamine and 1,2,3-triazole based benzaldehyde using a mixture of CH3CN/water as a reaction medium is described. The current protocol delivers numerous advantages such as good yield, short reaction time, easy work-up and simplicity in the procedure as it uses a green method and an eco-friendly catalyst. The target compounds are screened for their in-vitro anticancer activity and most of the compounds are found to exhibit promising activity compared to standard drug Doxorubicin. Molecular docking studies performed on caspase-3 and COVID-19 main protease revealed well defined binding interactions and docking scores.

Synthesis of 1,2,3‐Triazole‐Containing 2,3‐Dihydrofuran Derivatives, Evaluation of Anticancer Activity and Molecular Docking Studies



The benzofuranyl motif present in compounds exhibits various medicinal properties and
non-drug applications. These derivatives are naturally occurring compounds or synthetic materials,
which cover a broad spectrum of pharmacological activities like anti-inflammatory, anti-diabetic, anti-
depressant, anti-HIV, anti-microbial, anti-proliferative, anti-convulsant, cytotoxic, analgesic, etc.
Few of the commercially interesting compounds from this class are, ailanthoidol (anti-inflammatory),
amiodarone, dronedarone, celivarone (anti-arrhythmic), bufuralol (muscular airways relaxant), morphine,
5-(2-aminopropyl)benzofuran; 5-APB, 6-(2-aminopropyl)benzofuran; 6-APB (CNS), rifampicin
(antibiotic), etc., whereas, some of the non-drug applications are in perfumery industry (bergapten)
and as tannin activators in sunscreen preparations (psoralen, 8-methoxypsoralen, and angelicin).
Considering these interesting biological activities and commercial utilities, a review on the synthetic
aspects of this privileged scaffold was attempted. For the benefit of natural product-based drug discovery,
available sources of these derivatives, extraction process and reported biological activities
have also been outlined in this review.


Benzofuran: A Key Heterocycle - Ring Closure And Beyond

During a synthesis of coumarins to obtain new candidates for treating Alzheimer’s Disease (AD), an unusual rearrangement of a benzopyran group to a benzofuran group occurred, offering a novel synthesis pathway of these benzofuran derivatives. The possible mechanism of the novel rearrangement was also discussed. All of the benzofuran derivatives have weak anti-AChE activities compared with the reference compound, donepezil.

Synthesis of benzofuran derivatives via rearrangement and their inhibitory activity on acetylcholinesterase.

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Synthesis of benzofuran derivatives via rearrangement and their inhibitory activity on acetylcholinesterase.