An expedient synthesis and screening for antiacetylcholinesterase activity of piperidine embedded novel pentacyclic cage compounds

Med Chem. 2014 Mar;10(2):228-36. doi: 10.2174/157340641002140131170054.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / metabolism*
  • Aza Compounds / chemical synthesis
  • Aza Compounds / chemistry
  • Aza Compounds / pharmacology*
  • Cholinesterase Inhibitors / chemical synthesis
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / pharmacology*
  • Cyclopentanes / chemical synthesis
  • Cyclopentanes / chemistry
  • Cyclopentanes / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical*
  • Models, Molecular
  • Molecular Structure
  • Piperidines / chemistry*
  • Structure-Activity Relationship

Substances

  • Aza Compounds
  • Cholinesterase Inhibitors
  • Cyclopentanes
  • Piperidines
  • piperidine
  • Acetylcholinesterase