Synthesis of novel 7-benzylamino-2H-1, 4-benzoxazin-3 (4H)-ones as anticonvulsant agents

…, LP Guan, LM Zhao, HR Piao, ZS Quan

Index: Piao, Zhong-Tai; Guan, Li-Ping; Zhao, Li-Ming; Piao, Hu-Ri; Quan, Zhe-Shan European Journal of Medicinal Chemistry, 2008 , vol. 43, # 6 p. 1216 - 1221

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Citation Number: 15

Abstract

A series of 7-benzylamino-2H-1, 4-benzoxazin-3 (4H)-ones were synthesized using 2-amino- 5-nitrophenol as a starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES test) and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox.). The MES test showed that 7-(4-fluorobenzylamino)-2H-1, 4- benzoxazin-3 (4H)-one 4b was the most potent with ED50 value of 31.7 mg/kg and ...