Perspective Design of Chalcones for the Management of CNS Disorders: A Mini-Review

CNS Neurol Disord Drug Targets. 2019;18(6):432-445. doi: 10.2174/1871527318666190610111246.

Abstract

The development of chalcone-based compounds for CNS disorders has been explored by many research groups. Chalcones are being considered as a potent organic scaffold with widespread applications in the field of drug discovery and medicinal chemistry. The planar or semi-planar geometry of chalcones with various functionalities impinged on the terminal aromatic systems renders the molecule its bio-activity including anti-cancer, anti-malarial, anti-microbial, anti-fungal, antileishmanial, anti-viral, anti-diabetic, anti-hypertensive properties, etc. Moreover, cutting-edge research has been executed in the domain of Central Nervous System (CNS) based scheme, further, their identification and classifications also remain of high interest in the field of medicinal chemistry but the specific reviews are limited. Hence, the present review highlights the significance of chalcones toward their CNS activities (up to 2019), which include anti-depressant activity, anxiolytic activity, activity with GABA receptors, acetylcholinesterase (AChE) and butyryl cholinesterase (BChE) inhibitions, activity as adenosine receptor antagonists anti-Alzheimer's agents, β-amyloid plaques imaging agents, monoamine oxidase inhibition. To our knowledge, this is the first review exclusively for CNS activity profile of chalcones.

Keywords: Chalcones; GABA receptors; acetylcholinesterase (AChE); anti-Alzheimer’s agents; anti-depressant activity; anxiolytic activity; butyrylcholinesterase (BChE) inhibitions; monoamine oxidase inhibition; β-amyloid plaques imaging agents..

Publication types

  • Review

MeSH terms

  • Amyloid beta-Peptides / antagonists & inhibitors
  • Central Nervous System Diseases / drug therapy*
  • Chalcones / chemistry
  • Chalcones / pharmacology*
  • Cholinesterase Inhibitors / pharmacology*
  • Humans
  • Monoamine Oxidase Inhibitors / chemistry
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Amyloid beta-Peptides
  • Chalcones
  • Cholinesterase Inhibitors
  • Monoamine Oxidase Inhibitors