A review on coumarins as acetylcholinesterase inhibitors for Alzheimer's disease

Bioorg Med Chem. 2012 Feb 1;20(3):1175-80. doi: 10.1016/j.bmc.2011.12.042. Epub 2011 Dec 30.

Abstract

Acetylcholinesterase (AChE) enzyme inhibition is an important target for the management of Alzheimer disease (AD) and AChE inhibitors are the main stay drugs for its management. Coumarins are the phytochemicals with wide range of biological activities including AChE inhibition. The scientists have attempted to explore the coumarin template for synthesizing novel AChE inhibitors with additional pharmacological activities including decrease in beta-amyloid (Aβ) deposition and beta-secretase inhibition that are also important for AD management. Most of the designed schemes have involved incorporation of a catalytic site interacting moiety at 3- and 4-positions of the coumarin ring. The present review describes these differently synthesized coumarin derivatives as AChE inhibitors for management of AD.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acetylcholinesterase / metabolism
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / enzymology
  • Animals
  • Cholinesterase Inhibitors / chemistry*
  • Cholinesterase Inhibitors / pharmacology
  • Cholinesterase Inhibitors / therapeutic use*
  • Coumarins / chemistry*
  • Coumarins / pharmacology
  • Coumarins / therapeutic use*
  • Humans
  • Models, Molecular

Substances

  • Cholinesterase Inhibitors
  • Coumarins
  • Acetylcholinesterase