☆ 4.7 Article

Design & synthesis of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one as potential anticonvulsant agents

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2010)

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Volume 45, Issue 9, Pages 3960-3969

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

DOI: 10.1016/j.ejmech.2010.05.051

Keywords

[1,2,4] Triazin-6-one; Anticonvulsant; Behavioural test; Neurotoxicity; Computational parameter

Categories

Chemistry, Medicinal

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Abstract

A series of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one were designed & synthesized using appropriate synthetic route keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and CNS activities. After intraperitoneal injection to mice, some synthesized derivatives were examined in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol (scPTZ) induced seizure and neurotoxicity screens. Those found potent were also evaluated for behavioural impairment and depression activity. Among the compound tested, 5 eIX showed protection from seizures in both the animal models at dose level of 30 mg/kg while 5 bII & 5 cII showed protection against scPTZ model at same dose level. Some titled compounds exhibited lesser CNS depression and neurotoxicity compared to clinically effective drug. (C) 2010 Elsevier Masson SAS. All rights reserved.

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