Targeting GABA receptors with chalcone derivative compounds, what is the evidence?

Expert Opin Ther Targets. 2023 Jul-Dec;27(12):1257-1269. doi: 10.1080/14728222.2023.2293752. Epub 2023 Dec 30.

Abstract

Introduction: In medicinal chemistry, privileged structures have been frequently exploited as a successful template for drug discovery. Common simple scaffolds like chalcone are present in a wide range of naturally occurring chemicals. Chalcone exhibits extensive biological activity and has drawn attention in this context due to its function in the GABA receptor. Epilepsy and GABA receptors are related. It is a chronic neurological condition that affects globally.

Areas covered: Numerous neurological disorders, including anxiety and epilepsy, have been related to GABA, the brain's most prevalent inhibitory neurotransmitter. We go through the role of GABA receptors in anxiety and epilepsy in this review. The structure-activity relationship of chalcone and its derivatives on the GABA receptor is covered in our final section.

Expert opinion: GABA is a potential therapeutic target for issues associated with the nervous system. We talk about the potential effects of chalcone as a treatment for epilepsy and anxiety on the GABA receptor. Therefore, thorough research is necessary in this regard; the value of in silico tools in developing and enhancing GABA agonists is significant.

Keywords: GABA; GABA-A; GABA-B; anti-seizure; chalcone.

Publication types

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

MeSH terms

  • Chalcone* / chemistry
  • Chalcone* / pharmacology
  • Chalcones*
  • Epilepsy* / drug therapy
  • Humans
  • Receptors, GABA
  • Receptors, GABA-A / physiology
  • gamma-Aminobutyric Acid

Substances

  • Receptors, GABA
  • Chalcone
  • Chalcones
  • gamma-Aminobutyric Acid
  • Receptors, GABA-A