An Expedient Synthesis and Screening for Antiacetylcholinesterase Activity of Piperidine Embedded Novel Pentacyclic Cage Compounds

Author(s): Raju Suresh Kumar, Abdulrahman I. Almansour, Natarajan Arumugam, Hasnah Osman, Mohamed Ashraf Ali, Alireza Basiri, Yalda Kia.

Journal Name: Medicinal Chemistry

Volume 10 , Issue 2 , 2014

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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.

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Article Details

VOLUME: 10
ISSUE: 2
Year: 2014
Page: [228 - 236]
Pages: 9
DOI: 10.2174/157340641002140131170054
Price: $58

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