Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

doi:10.3390/molecules17054811

Paper

Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

Published Apr 25, 2012 · M. M. Ismail, M. Kamel, L. W. Mohamed

Molecules

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Abstract

New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl) piperazin-1-yl)acetyl)indoline-2,3-dione (IIId) was found to be the most potent.

In Vitro Study

Study Snapshot

New indole derivatives, like 1-(2-(4-(2-fluorobenzyl) piperazin-1-yl)acetyl)indoline-2,3-dione (IIId), show potent acetylcholinesterase inhibitor activity, with the most

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

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References

BZYX, a novel acetylcholinesterase inhibitor, significantly improved chemicals-induced learning and memory impairments on rodents and protected PC12 cells from apoptosis induced by hydrogen peroxide.

BZYX improves memory impairments in rodents and protects PC12 cells from apoptosis induced by hydrogen peroxide, making it a potential candidate for neurodegenerative disease intervention.

Interactions between the amyloid and cholinergic mechanisms in Alzheimer's disease

Alzheimer's disease is linked to both amyloid- build-up and cholinergic dysfunction, with bidirectional pathways linking these two hypotheses.

Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues.

Novel coumarin analogues with substitution on positions 3 and 4 show parallel anti-acetylcholinesterase activities compared to the reference compound donepezil.

Acetylcholinesterase inhibitors: novel activities of old molecules.

Acetylcholinesterase inhibitors show potential in modulating amyloid precursor protein processing through complex mechanisms, potentially improving cognitive function in Alzheimer's disease patients.

Synthesis and biological evaluation as AChE inhibitors of new indanones and thiaindanones related to donepezil.

New indanones and thiaindanones related to donepezil show potential as AChE inhibitors, with the best compound showing inhibitory activity in the same range as donepezil.

Citations

Indole analogs as potential anti-breast cancer agents: Design, synthesis, in-vitro bioevaluation with DFT, molecular docking and ADMET studies

Indole hybrids with halogen substituents show potential as anti-breast cancer agents, particularly against triple-negative breast cancer.

Synthesis of indole-functionalized isoniazid conjugates with potent antimycobacterial and antioxidant efficacy.

Indole-isoniazid conjugates show promising antimycobacterial and antioxidant efficacy, making them potential leads for developing anti-TB medications with synergetic antioxidant action.

Assessing Indole Derivative Molecules as Dual Acetylcholinesterase and Butyrylcholinesterase Inhibitors through In Vitro Inhibition and Molecular Modelling Studies

Indole derivatives show strong inhibition effects on both acetylcholinesterase and butyrylcholinesterase, suggesting potential for new Alzheimer's disease treatments with fewer side effects.

Design, synthesis, in vitro and in silico evaluations of new isatin-triazine- aniline hybrids as potent anti- Alzheimer multi-target directed lead compounds.

New isatin-triazine- aniline hybrids show potential as potent anti-Alzheimer's disease compounds with good anticholinesterase, antioxidant, and biometal chelation abilities.

Enzyme inhibitory potential of some indole Schiff bases on acetylcholinesterase and human carbonic anhydrase isoforms I and II enzymes: an in vitro and molecular docking study.

Indole Schiff base compounds significantly inhibit acetylcholinesterase and human carbonic anhydrase enzymes, with 1k and 1p showing the best inhibitory effects for hCAI and 1p for hCAII.

An Efficient One-Pot Synthesis of Acenaphtho[1,2-b]indolindeneone and Acenaphtho[1,2-b]indoldione Derivatives

This study presents a simple, environmentally friendly, and high-yield method for synthesis of acenaphtho[1,2-b]indolindenedione and acenaphtho[1,2-b]indolone derivatives using a four-component reaction

SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL HETERONUCLEAR BIS-THIAZOLIDINONE DERIVATIVES AND EVALUATION OF ITS ANTIMICROBIAL AND IN VITRO CYTOTOXIC PROPERTY

The synthesized novel bis-thiazolidinone derivatives show no antimicrobial or in vitro cytotoxic activity against bacteria or fungi, but show potential as antifungal agents.