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

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
• chalcone
• anti-seizure

Article highlights

• Chalcones are chemically α,β-unsaturated ketones

• Chalcones play a crucial role in the binding of GABA receptor

• The presence of hydroxyl, methoxy and chlorine groups on chalcones is favorable for the GABA action

• Chalcones are considered the lead framework for the development of Antiseizure drugs

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This article was funded King Khalid University through Research Center for Advanced Materials Science (RCAMS) under [grant no: RCAMS/KKU/001-23].