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

作者：Kumar Raju Suresh^*; Almansour Abdulrahman I; Arumugam Natarajan; Osman Hasnah; Ali Mohamed Ashraf; Basiri Alireza; Kia Yalda

来源：Medicinal Chemistry, 2014, 10(2): 228-236.

DOI：10.2174/157340641002140131170054

• Alzheimer%26apos
• s disease
• AChE inhibitor
• 1,3-Dipolar cycloaddition
• azomethine ylide
• diazapentacycles and microwave irradiation

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 mu M and this may provide a new lead for developing potential inhibitors for Alzheimer%26apos;s disease.

• 出版日期2014-3