Acetylcholinesterase Enzyme Inhibitor Molecules with Therapeutic Potential for Alzheimer's Disease

CNS Neurol Disord Drug Targets. 2022;21(5):427-449. doi: 10.2174/1871527320666210928160159.

Abstract

Acetylcholinesterase (AchE), hydrolase enzyme, regulates the hydrolysis of acetylcholine neurotransmitter in the neurons. AchE is found majorly in the central nervous system at the site of cholinergic neurotransmission. It is involved in the pathophysiology of Alzheimer's diseasecausing dementia, cognitive impairment, behavioral and psychological symptoms. Recent findings involved the inhibition of AchE that could aid in the treatment of Alzheimer's. Many drugs of different classes are being analyzed in the clinical trials and examined for their potency. Drugs that are used in the treatment of Alzheimer's disease are donepezil, galantamine, tacrine, rivastigmine showing major adverse effects. To overcome this, researchers work on novel drugs to elicit inhibition. This review comprises many hybrids and non-hybrid forms of heteroaromatic and nonheteroaromatic compounds that were designed and evaluated for AchE inhibition by Ellman's method of assay. These novel compounds may assist future perspectives in the discovery of novel moieties against Alzheimer's disease by the inhibition of AchE.

Keywords: Acetylcholinesterase; Ellman’s assay; docking; donepezil; hybrid molecules; rivastigmine.

Publication types

  • Review

MeSH terms

  • Acetylcholinesterase
  • Alzheimer Disease* / drug therapy
  • Cholinesterase Inhibitors* / pharmacology
  • Cholinesterase Inhibitors* / therapeutic use
  • Donepezil / therapeutic use
  • Humans
  • Rivastigmine / pharmacology
  • Rivastigmine / therapeutic use

Substances

  • Cholinesterase Inhibitors
  • Donepezil
  • Acetylcholinesterase
  • Rivastigmine