Synthesis of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles as potential anticonvulsant agents期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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Synthesis of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles as potential anticonvulsant agents

Authors:	Cheng-Xi Wei Di Wu Zhi-Gang Sun Kyu-Yun Chai Zhe-Shan Quan

Institution:	(1) Institute of Neurosurgery, Inner Mongolia University for Nationalities, No. 1742, Holin River Street, Tongliao, Inner Mongolia Autonomous Region, 028007, People’s Republic of China;(2) College of Pharmacy, Yanbian University, No. 121, JuZi Street, Yanji, Jilin, 133000, People’s Republic of China;(3) Department of Chemistry, Wonkwang University, Iksan, 570-749, Korea;

Abstract:	A series of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzod]oxazoles was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazole (Sc-PTZ), and rotarod tests in intraperitoneally injected mice. Among the synthesized compounds, compound 2-phenyl-6-(4H-1,2,4-triazol-4-yl)benzod]oxazole (3a) could be considered the potentially most useful and safe therapeutic compound, with ED₅₀ = 29.6 mg/kg, TD₅₀ = 285 mg/kg, and PI = 9.7. Its neurotoxicity was the lowest of all the synthesized compounds and was also markedly lower than that of the reference drug carbamazepine with PI value of 6.4.

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