An ongoing journey of chalcone analogues as single and multi-target ligands in the field of Alzheimer's disease: A review with structural aspects

Life Sci. 2023 May 1:320:121568. doi: 10.1016/j.lfs.2023.121568. Epub 2023 Mar 15.

Abstract

Alzheimer's disease (AD) is a chronic and irreversible neurodegenerative disorder with progressive dementia and cognitive impairment. AD poses severe health challenge in elderly people and become one of the leading causes of death worldwide. It possesses complex pathophysiology with several hypotheses (cholinergic hypothesis, amyloid hypothesis, tau hypothesis, oxidative stress, mitochondrial dysfunction etc.). Several attempts have been made for the management of multifactorial AD. Acetylcholinesterase is the only target has been widely explored in the management of AD to the date. The current review set forth the chalcone based natural, semi-synthetic and synthetic compounds in the search of potential anti-Alzheimer's agents. The main highlights of current review emphasizes on chalcone target different enzymes and pathways like Acetylcholinesterase, β-secretase (BACE1), tau proteins, MAO, free radicals, Advanced glycation end Products (AGEs) etc. and their structure activity relationships contributing in the inhibition of above mentioned various targets of AD.

Keywords: AChE; AGEs; Alzheimer's disease; Amyloid beta; Antioxidants; BACE-1; Chalcone; MAO-B.

Publication types

  • Review

MeSH terms

  • Acetylcholinesterase / metabolism
  • Aged
  • Alzheimer Disease* / drug therapy
  • Alzheimer Disease* / metabolism
  • Amyloid Precursor Protein Secretases / metabolism
  • Amyloid beta-Peptides / metabolism
  • Aspartic Acid Endopeptidases
  • Chalcones*
  • Humans
  • Ligands

Substances

  • Acetylcholinesterase
  • Amyloid Precursor Protein Secretases
  • Chalcones
  • Aspartic Acid Endopeptidases
  • Amyloid beta-Peptides
  • Ligands