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Xian-Qing Deng, Ming-Xia Song, Cheng-Xi Wei, Zhi-Gang Sun, Zhe-Shan Quan. Synthesis and evaluation of 7-substituted-3,4-dihydrobenzo[1,4]oxazepin-5(2H)-ones as anticonvulsant and hypnotic agents. MED CHEM RES. 2011, 20 (7):996-1004.
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Synthesis and evaluation of 7-substituted-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-ones as anticonvulsant and hypnotic agents


×÷Õßeng, XQ (Deng, Xian-Qing)[ 1 ] ; Song, MX (Song, Ming-Xia)[ 1 ] ; Wei, CX (Wei, Cheng-Xi)[ 2 ] ; Sun, ZG (Sun, Zhi-Gang)[ 2 ] ; Quan, ZS (Quan, Zhe-Shan)[ 1 ]




MEDICINAL CHEMISTRY RESEARCH



¾í: 20

ÆÚ: 7

Ò³: 996-1004

DOI: 10.1007/s00044-010-9434-y

³ö°æÄê: SEP 2011

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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 (ED(50)) 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.


¹Ø¼ü´Ê

×÷Õ߹ؼü´Ê:1,4-Benzoxazepin-5(2H)-one; Synthesis; Anticonvulsant; Maximal electroshock; Hypnosis

KeyWords Plus:ANTIEPILEPTIC DRUG DEVELOPMENT; EPILEPSY


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ͨѶ×÷ÕßµØÖ·: Quan, ZS (ͨѶ×÷Õß)





Yanbian Univ, Coll Pharm, 977 Pk Rd, Yanji 133002, Jilin, Peoples R China.





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[ 1 ] Yanbian Univ, Coll Pharm, Yanji 133002, Jilin, Peoples R China





      

[ 2 ] Inner Mongolia Univ Nationalities, Inst Neurosurg, Tongliao 028007, Inner Mongolia, Peoples R China



µç×ÓÓʼþµØÖ·:sunzhigang101@yahoo.cn; zsquan@ybu.edu.cn


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National Natural Science Foundation of China


30860340

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BIRKHAUSER BOSTON INC, 675 MASSACHUSETTS AVE, CAMBRIDGE, MA 02139 USA


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Web of Science Àà±ð:Chemistry, Medicinal


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ÓïÖÖ:English

Èë²ØºÅ: WOS:000293296500021

ISSN: 1054-2523


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IDS ºÅ: 799OR

Web of Science ºËÐĺϼ¯ÖÐµÄ "ÒýÓõIJο¼ÎÄÏ×": 14

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Mahdavi, Mohammad. Synthesis of Novel Benzo[6,7][1,4] oxazepino[4,5-a] quinazolinone Derivatives via Transition-Metal-Free Intramolecular Hydroamination. SYNLETT, FEB 13 2014.



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Synthesis of Novel Benzo[6,7][1,4] oxazepino[4,5-a] quinazolinone Derivatives via Transition-Metal-Free Intramolecular Hydroamination

×÷Õß: Mahdavi, Mohammad; Foroughi, Niloufar; Saeedi, Mina; µÈ.

SYNLETT  ¾í: 25   ÆÚ: 3   Ò³: 385-388   ³ö°æÄê: FEB 13 2014
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