Synthesis and biological evaluation of 3-arylcoumarins as potential anti-Alzheimer's disease agents

J Enzyme Inhib Med Chem. 2019 Dec;34(1):651-656. doi: 10.1080/14756366.2019.1574297.


Alzheimer's disease, a neurodegenerative illness, has the extremely complex pathogenesis. Accumulating evidence indicates there is a close relationship between several enzymes and Alzheimer's disease. Various substituted 3-arylcoumarin derivatives were synthesised, and their in vitro activity, including cholinesterase inhibitory activity, monoamine oxidase inhibitory activity, and antioxidant activity were investigated. Most of the compounds exhibited high activity; therefore 3-arylcoumarin compounds have the potential as drug candidates for the treatment of Alzheimer's disease.

Keywords: 3-Arylcoumarin; Alzheimer’s disease; antioxidant activity; cholinesterase inhibitors; monoamine oxidase inhibitors.

MeSH terms

  • Acetylcholinesterase / metabolism*
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / metabolism
  • Animals
  • Antioxidants / chemical synthesis
  • Antioxidants / chemistry
  • Antioxidants / pharmacology*
  • Cholinesterase Inhibitors / chemical synthesis
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / pharmacology*
  • Coumarins / chemical synthesis
  • Coumarins / chemistry
  • Coumarins / pharmacology*
  • Dose-Response Relationship, Drug
  • Molecular Structure
  • Monoamine Oxidase / metabolism*
  • Monoamine Oxidase Inhibitors / chemical synthesis
  • Monoamine Oxidase Inhibitors / chemistry
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Rats, Wistar
  • Structure-Activity Relationship
  • Zebrafish


  • Antioxidants
  • Cholinesterase Inhibitors
  • Coumarins
  • Monoamine Oxidase Inhibitors
  • Monoamine Oxidase
  • Acetylcholinesterase

Grants and funding

The authors are grateful to support from the Science and Technology Research Programme of Shandong Academy of Medical Sciences (2017–16), Shandong Provincial Natural Science Foundation [ZR2018LH021] and the Innovation Project of Shandong Academy of Medical Sciences.