Drug intelligence / Profile preview

n-(4-(3-(4-bromophenyl)acryloyl)phenyl)-4-(trifluoromethyl)benzenesulfonamide

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

n-(4-(3-(4-bromophenyl)acryloyl)phenyl)-4-(trifluoromethyl)benzenesulfonamide is a synthetic small molecule sulfonamide-chalcone hybrid investigated as a potential antiepileptic drug (AED). It belongs to a series of sulfonamide-chalcone derivatives designed to modulate the γ-aminobutyric acid type A (GABAA) receptor, the primary inhibitory neurotransmitter system in the central nervous system. The compound functions as a positive allosteric modulator (PAM) of the GABAA receptor, enhancing GABAergic inhibition to control neuronal hyperexcitability and suppress seizures. In preclinical studies, this specific 4-bromophenyl derivative was identified as one of the most promising candidates in its series (likely identified as Compound 21), demonstrating high binding affinity to the GABAA receptor in molecular docking and molecular dynamics simulations. Its safety profile and anticonvulsant efficacy have been validated in vivo using pentylenetetrazole (PTZ)-induced seizure models in zebrafish.

Other names
n-(4-(3-(4-bromophenyl)acryloyl)phenyl)-4-(trifluoromethyl)benzenesulfonamide4-(trifluoromethyl)-N-(4-(3-(4-bromophenyl)acryloyl)phenyl)benzenesulfonamide
02

Targets

GABRR (GABA-A receptor subunit rho)

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