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

Feba Benny,Sunil Kumar, Aiswarya Binu,Della Grace Thomas Parambi, Tariq G. Alsahli,Abdullah G. Al-Sehemi, Namitha Chandran, Deepthi S. Manisha, Sarath Sreekumar,Akanksha Bhatt,Krishnadas Madhu,Bijo Mathew

EXPERT OPINION ON THERAPEUTIC TARGETS(2023)

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摘要
IntroductionIn 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 coveredNumerous 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 opinionGABA 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.
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关键词
GABA,GABA-A,GABA-B,chalcone,anti-seizure
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