Design and Synthesis of Benzotriazole Derivatives for Anti-convulsant Activity
Year: 2025
Type: article
Abstract: Design and Synthesis of Benzotriazole Derivatives for Anticonvulsant Activity Epilepsy is a prevalent neurological disorder significantly impacting global health and economy, necessitating the development of novel therapeutic agents. Benzotriazole derivatives, known for their diverse biological activities, present a promising scaffold for new antiepileptic drugs. This study aimed to synthesize novel benzotriazole-linked triazine derivatives, characterize their physicochemical properties, and evaluate their potential anticonvulsant activity through in silico ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) and docking studies, as well as in vivo maximal electroshock seizure (MES) model testing. Our approach involved a five-step synthesis of five benzotriazole derivatives (PTB1-5), including the formation of benzotriazole, N-esterification, nucleophilic substitution, cyclization to triazine, and Schiff's base formation. Characterization was performed using melting point, solubility, and spectral analysis (¹H-NMR, FT-IR). In silico studies predicted drug-likeness and ADMET properties . Anticonvulsant activity was assessed in Wistar albino rats using the MES model, observing hind limb extension and clonus. Results showed that compounds PTB1, PTB2, and PTB5 significantly reduced the onset of hind limb extension in the MES model, demonstrating considerable anticonvulsant action. PTB3 and PTB4 also showed reduction in onset. All synthesized compounds exhibited good drug-likeness and favorable ADMET properties, with high intestinal absorption. Docking studies indicated binding affinity to the GABA-AT receptor, suggesting a potential mechanism of action In conclusion, this research successfully synthesized novel benzotriazole-linked triazine derivatives with promising anticonvulsant activity and favorable pharmacokinetic profiles, warranting further investigation as potential antiepileptic drug candidates.
Author: Praduman Kumar Pandit, Priyal Jain*
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W6893521688
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