Abstract
The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12±0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.
Keywords: Alzheimer's disease, AChE inhibitor, 1, 3-Dipolar cycloaddition, azomethine ylide, diazapentacycles and microwave irradiation.
Medicinal Chemistry
Title:An Expedient Synthesis and Screening for Antiacetylcholinesterase Activity of Piperidine Embedded Novel Pentacyclic Cage Compounds
Volume: 10 Issue: 2
Author(s): Raju Suresh Kumar, Abdulrahman I. Almansour, Natarajan Arumugam, Hasnah Osman, Mohamed Ashraf Ali, Alireza Basiri and Yalda Kia
Affiliation:
Keywords: Alzheimer's disease, AChE inhibitor, 1, 3-Dipolar cycloaddition, azomethine ylide, diazapentacycles and microwave irradiation.
Abstract: The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12±0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.
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Kumar Suresh Raju, Almansour I. Abdulrahman, Arumugam Natarajan, Osman Hasnah, Ali Ashraf Mohamed, Basiri Alireza and Kia Yalda, An Expedient Synthesis and Screening for Antiacetylcholinesterase Activity of Piperidine Embedded Novel Pentacyclic Cage Compounds, Medicinal Chemistry 2014; 10 (2) . https://dx.doi.org/10.2174/157340641002140131170054
DOI https://dx.doi.org/10.2174/157340641002140131170054 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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