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

[ Vol. 10 , Issue. 2 ]

Author(s):

Raju Suresh Kumar, Abdulrahman I. Almansour, Natarajan Arumugam, Hasnah Osman, Mohamed Ashraf Ali, Alireza Basiri and Yalda Kia   Pages 228 - 236 ( 9 )

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 µ M 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.

Affiliation:

Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.



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