Synthesis and Molecular Docking Study of Some New 4-{[4-(2-Furoyl)-1-piperazinyl]methyl}-N-(substituted-phenyl)benzamides as PossibleTherapeutic Entrants for Alzheimers Disease

doi:10.4172/2161-0444.1000337

Paper

Synthesis and Molecular Docking Study of Some New 4-{[4-(2-Furoyl)-1-piperazinyl]methyl}-N-(substituted-phenyl)benzamides as PossibleTherapeutic Entrants for Alzheimers Disease

Published Feb 29, 2016 · G. Hussain, M. Abbasi, A. Rehman

Medicinal Chemistry

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Abstract

In the present work, a new series of different 4-{[4-(2-furoyl)-1-piperazinyl]methyl}-N-(substituted-phenyl) benzamides (5a-h) have been synthesized as possible therapeutic agents for the treatment of Alzheimer’s disease. The structural confirmation of all the synthesized compounds was carried out by their IR, 1H-NMR and EI-MS spectral data. Enzyme inhibition activity was performed against butyrylcholinestrase enzyme, which revealed that, 4-{[4-(2-furoyl)-1- piperazinyl]methyl}-N-(4-ethylphenyl)benzamide (5b) showed excellent IC50 value 0.82 ± 0.001 μM relative to Eserine, a reference standard having IC50 value of 0.85 ± 0.0001 μM. The enhanced potential of this molecule may be attributed to the 4-ethylphenyl group. As the cholinesterase enzyme inhibitors are good targets for Alzheimer’s disease, therefore, the inhibition study of these synthesized molecules was carried out to discover their possible therapeutic effect as target for aforesaid disease.

In Vitro Study

Study Snapshot

New 4-[4-(2-furoyl)-1-piperazinyl]methyl-N-(substituted-phenyl)benzamides show potential as Alzheimer's disease treatments due to their cholinesterase enzyme inhibitory activity.

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 and Molecular Docking Study of Some New 4-{[4-(2-Furoyl)-1-piperazinyl]methyl}-N-(substituted-phenyl)benzamides as PossibleTherapeutic Entrants for Alzheimers Disease

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Citations

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