Synthesis and evaluation of 7-substituted-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-ones as anticonvulsant and hypnotic agents

作者：Deng, Xian-Qing; Song, Ming-Xia; Wei, Cheng-Xi; Sun, Zhi-Gang; Quan, Zhe-Shan^*

来源：Medicinal Chemistry Research, 2011, 20(7): 996-1004.

DOI：10.1007/s00044-010-9434-y

• 1,4-Benzoxazepin-5(2H)-one
• Synthesis
• Anticonvulsant
• Maximal electroshock
• Hypnosis

A series of 7-substituted-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-ones was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were evaluated with a maximal electroshock (MES) test and a rotated test in mice, respectively. Most of the compounds prepared exhibited anticonvulsant activities in the MES test, 7-(heptyloxy)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one (10) was the most active. In the anti-MES potency test, it showed a median effective dose (ED50) of 19.0 mg/kg. The hypnotic effect of the compound 10 was initially investigated by using a pentobarbital-induced-sleep test. Middle (30 mg/kg) and high doses (60 mg/kg) of the compound 10 both significantly increased the pentobarbital-induced sleep from 20.9 +/- A 5.28 to 26.9 +/- A 6.14 and 45.67 +/- A 7.94 min, respectively.

• 单位
  内蒙古民族大学; 延边大学