Medicinal Chemistry

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

DOI: 10.2174/157340641002140131170054

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

Page: [228 - 236] Pages: 9

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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.