Potent acetylcholinesterase inhibitors: design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives.

doi:10.1016/j.ejmech.2015.01.044

Paper

Potent acetylcholinesterase inhibitors: design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives.

Published Mar 6, 2015 · M. Mohammadi‐Khanaposhtani, Mina Saeedi, Narges Shamsaei Zafarghandi

European journal of medicinal chemistry

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Abstract

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In Vitro Study

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Study Snapshot

A novel series of acridone linked to 1,2,3-triazole derivatives has been synthesized, with 10-((1-(4-chlorobenzyl)-1 H-1,2,3-triazol-4-yl)methyl)-2-methoxyacridin-9(10

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Potent acetylcholinesterase inhibitors: design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives.

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References

Indolinone-based acetylcholinesterase inhibitors: synthesis, biological activity and molecular modeling.

Indolinone-based compounds with benzylpyridinium moiety show potent inhibitory activity against acetylcholinesterase, with 2-chlorobenzyl derivative 3c being 32-fold more potent than standard drug donepezil.

A new roadmap for drug development for Alzheimer's disease

Alzheimer's disease drug development trials lack four important deficiencies, limiting our understanding of neuropathologies, drug effectiveness, and disease modification.

Novel coumarin-3-carboxamides bearing N-benzylpiperidine moiety as potent acetylcholinesterase inhibitors.

Compound 10c, a novel coumarin-3-carboxamide derivative with an N-benzylpiperidine moiety, is 46-fold more potent than standard drug donepezil and exhibits mixed-type inhibition against acetylcholinesterase.

Design, synthesis, biological evaluation and docking study of 5-oxo-4,5-dihydropyrano[3,2-c]chromene derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.

The 1-(4-fluorobenzyl)pyridinium derivative 6g shows the most potent anti-AChE activity and highest AChE/BuChE selectivity, with potential binding modes.

Two new acridone alkaloids from the branch of Atalantia buxifolia and their biological activity

Two new acridone alkaloids from Atalantia buxifolia show significant antibacterial activity against Staphylococcus aureus and weak inhibitory effect on acetylcholinesterase.

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