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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

A New Class of Anticonvulsants Possessing 6 Hz Psychomotor Seizure Test Activity: 2-(1H-Benzotriazol-1-yl)-N'-[Substituted] Acetohydrazides

Author(s): Praveen Kumar and Laxmi Tripathi

Volume 8, Issue 3, 2012

Page: [337 - 348] Pages: 12

DOI: 10.2174/157340612800786606

Price: $65

Abstract

A series of 2-(1H-Benzotriazol-1-yl)-N'-[substituted]acetohydrazides were designed & synthesized keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and neurotoxicity. The new compounds were characterized using FT-IR, 1H NMR, mass spectral data and elemental analysis. The anticonvulsant activity of the titled compounds was assessed using the 6 Hz psychomotor seizure test. The neurotoxicity was assessed using the rotorod method. The most active compound of the series was N'-[4-(1,3-Benzodioxol-5-yloxy)benzylidene]-2-(1H-benzotriazol-1-yl)acetohydrazide (BTA 9), which showed good activity with 75 % protection (3/4, 0.5 h) at a dose of 100 mg/kg in mice. All the compounds exhibited no neurotoxicity. A computational study was carried out for calculation of pharmacophore pattern and prediction of pharmacokinetic properties. Titled compounds have also exhibited good binding properties with epilepsy molecular targets such as glutamate, GABA (A) delta, GABA (A) alpha-1 receptors and Na/H exchanger, in Lamarckian genetic algorithm based flexible docking studies.

Keywords: Anticonvulsant, Benzotriazole, Computational study, Docking study, 6 Hz Psychomotor Seizure test, Neurotoxicity, Lamarckian, acetohydrazides, epidemiological, Flavivirade


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