Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones

Cent Nerv Syst Agents Med Chem. 2019;19(1):67-71. doi: 10.2174/1871524918666181119114016.

Abstract

Background: Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD).

Methods: The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.

Results: Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively.

Conclusion: Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.

Keywords: Acetylcholinesterase; butyrylcholinesterase; chalcone; docking; monoamine oxidase-B; thiophene..

Publication types

  • Letter

MeSH terms

  • Acetylcholinesterase / metabolism
  • Animals
  • Chalcones / chemistry*
  • Chalcones / pharmacology
  • Cholinesterase Inhibitors / chemistry*
  • Cholinesterase Inhibitors / pharmacology
  • Crystallography, X-Ray
  • Horses
  • Humans
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / chemistry*
  • Monoamine Oxidase Inhibitors / pharmacology
  • Structure-Activity Relationship

Substances

  • Chalcones
  • Cholinesterase Inhibitors
  • Monoamine Oxidase Inhibitors
  • Monoamine Oxidase
  • Acetylcholinesterase