Abstract
Introduction: A novel series of multifunctional anti-Alzheimer’s agents based on Nsubstituted aryl sulphonamides were designed and synthesized. During in vivo moderate to good anti- Alzheimer’s Disease (AD) activity was observed as correlated by the modulation of some selected biochemical markers of AD as well as during behavioral assessment.
Methods: Among the series, some compounds have shown multi-functional potency by inhibition of Acetylcholinesterase (AChE), Scopolamine induced oxidative stress and were found comparable to the standard drug. Successful modulation of biochemical markers of oxidative stress in AD, displays neuroprotective properties and did not exert any significant toxicity.
Results and Conclusion: Thus, the present study has evidently shown that these series of compounds have potential to be optimized as anti-AD agents with multi-functional properties. The aryl sulphonamide nucleus might serve as a promising lead candidate for developing novel anti-AD drug.
Keywords: Alzheimer`s disease, behavioral assessment, oxidative stress, Acetylcholinesterase (AChE), inhibition, histopathology.
Graphical Abstract
Current Computer-Aided Drug Design
Title:N-Substituted Aryl Sulphonamides as Potential Anti-Alzheimer’s Agents: Design, Synthesis and Biological Evaluation
Volume: 14 Issue: 4
Author(s): Neeraj Masand*, Satya P. Gupta and Ratan Lal Khosa
Affiliation:
- Department of Pharmacy, Lala Lajpat Rai Memorial Medical College, Meerut, Uttar Pradesh,India
Keywords: Alzheimer`s disease, behavioral assessment, oxidative stress, Acetylcholinesterase (AChE), inhibition, histopathology.
Abstract: Introduction: A novel series of multifunctional anti-Alzheimer’s agents based on Nsubstituted aryl sulphonamides were designed and synthesized. During in vivo moderate to good anti- Alzheimer’s Disease (AD) activity was observed as correlated by the modulation of some selected biochemical markers of AD as well as during behavioral assessment.
Methods: Among the series, some compounds have shown multi-functional potency by inhibition of Acetylcholinesterase (AChE), Scopolamine induced oxidative stress and were found comparable to the standard drug. Successful modulation of biochemical markers of oxidative stress in AD, displays neuroprotective properties and did not exert any significant toxicity.
Results and Conclusion: Thus, the present study has evidently shown that these series of compounds have potential to be optimized as anti-AD agents with multi-functional properties. The aryl sulphonamide nucleus might serve as a promising lead candidate for developing novel anti-AD drug.
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Cite this article as:
Masand Neeraj *, Gupta P. Satya and Khosa Lal Ratan , N-Substituted Aryl Sulphonamides as Potential Anti-Alzheimer’s Agents: Design, Synthesis and Biological Evaluation, Current Computer-Aided Drug Design 2018; 14 (4) . https://dx.doi.org/10.2174/1573409914666180604115425
DOI https://dx.doi.org/10.2174/1573409914666180604115425 |
Print ISSN 1573-4099 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6697 |
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