Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues

Bioorg Med Chem. 2008 Sep 1;16(17):8011-21. doi: 10.1016/j.bmc.2008.07.068. Epub 2008 Jul 29.

Abstract

Three series (series A-C) of coumarin analogues with phenylpiperazine functions as substitution were designed and synthesized for studying their potential for treating Alzheimer's (AD) disease. Their anticholinesterase activities were assayed according to Ellmann's method against freshly prepared acetylcholinesterase (AChE) from Electrophorus electricus using donepezil as the reference compound. Pharmacological study and preliminary structure-activity relationships showed that coumarins with substitution on positions 3 and/or 4 have parallel anti-AchE activities compared with the reference compound.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / drug effects*
  • Cholinesterase Inhibitors / chemical synthesis
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / pharmacology*
  • Coumarins / chemical synthesis
  • Coumarins / chemistry
  • Coumarins / pharmacology*
  • Drug Design*
  • Drug Evaluation, Preclinical
  • Enzyme Activation / drug effects
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Cholinesterase Inhibitors
  • Coumarins
  • Acetylcholinesterase