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Xian-Qing Deng, Li-Na Quan, Cheng-Xi Wei, and Zhe-Shan Quan.  Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives.  EUR J MED CHEM, 2011, 46:2955-63.
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dengxianqing: 金币+3, ★★★★★最佳答案 2014-09-20 12:50:53
oven1986: LS-EPI+1, 感谢应助! 2014-09-21 00:36:38
2楼2014-09-20 12:01:54
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dengxianqing: 金币+3, ★★★很有帮助 2014-09-20 12:51:30
Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4] triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives


作者eng, XQ (Deng, Xian-Qing)[ 1 ] ; Quan, LN (Quan, Li-Na)[ 1 ] ; Song, MX (Song, Ming-Xia)[ 1 ] ; Wei, CX (Wei, Cheng-Xi)[ 2 ] ; Quan, ZS (Quan, Zhe-Shan)[ 1 ]




EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY



卷: 46

期: 7

页: 2955-2963

DOI: 10.1016/j.ejmech.2011.04.020

出版年: JUL 2011

查看期刊信息





























摘要

Herein, we described the syntheses and anticonvulsant activities of 7-(substituted-phenyl)-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones (1a-1o) and their derivatives. Most of the synthesized compounds exhibited potent anticonvulsant activities in the maximal electroshock test (MES). The most promising compound 1i showed significant anticonvulsant activity in MES test with ED(50) value of 19.7 mg/kg. It displayed a wide margin of safety with protective index much higher than the standard drugs. In addition, the potence of compound 1i against seizures induced by Pentylenetetrazole, Isoniazid, Thiosemicarbazide, 3-Mercaptopropionic acid, and Bicuculline in the chemical-induced seizure tests suggested that compound 1i displayed broad spectrum activity in several models, and it is likely to have several mechanisms of action including inhibiting voltage-gated ion channels and modulating GABAergic activity. (C) 2011 Elsevier Masson SAS. All rights reserved.


关键词

作者关键词:Synthesis; Anticonvulsant; Triazolo[1,5-a]pyrimidin; Imidazo[1,2-a]pyrimidin; Pyrazolo[1,5-a]pyrimidin; Maximal electroshock

KeyWords Plus:ANTIEPILEPTIC DRUGS; EPILEPSY; GABA; ANTAGONISM; SEIZURES; DESIGN


作者信息

通讯作者地址: Quan, ZS (通讯作者)





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





地址:





[ 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



电子邮件地址:weichengxi1224@yahoo.com.cn; zsquan@ybu.edu.cn


基金资助致谢



基金资助机构

授权号



National Natural Science Foundation of China


30860340

查看基金资助信息   




出版商

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 23 RUE LINOIS, 75724 PARIS, FRANCE


类别 / 分类

研究方向harmacology & Pharmacy

Web of Science 类别:Chemistry, Medicinal


文献信息

文献类型:Article

语种:English

入藏号: WOS:000291895200033

ISSN: 0223-5234


期刊信息


Impact Factor (影响因子): Journal Citation Reports®


其他信息

IDS 号: 780XS

Web of Science 核心合集中的 "引用的参考文献": 31

Web of Science 核心合集中的 "被引频次": 5









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3楼2014-09-20 12:02:07
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dengxianqing: 金币+1, ★★★很有帮助 2014-09-20 12:51:38
入藏号: WOS:000291895200033
4楼2014-09-20 12:02:21
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dengxianqing: 金币+1, ★★★很有帮助 2014-09-20 12:51:56
被引频次: 5
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Partially hydrogenated 2-amino [1,2,4]triazolo[1,5-a]pyrimidines as synthons for the preparation of polycondensed heterocycles: reaction with chlorocarboxylic acid chlorides

作者: Chernyshev, Victor M.; Pyatakov, Dmitry A.; Sokolov, Andrey N.; 等.

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Preparation and antimicrobial activity evaluation of some new bi- and triheterocyclic azoles

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Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines

作者: Zheng, Yan; Bian, Ming; Deng, Xian-Qing; 等.

ARCHIV DER PHARMAZIE  卷: 346   期: 2   页: 119-126   出版年: FEB 2013

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Synthesis and Anticonvulsant Activity Evaluation of Some 1-alkoxy-4-(1H-1,2,4-triazol-1-yl)phthalazines

作者: Wang, Shi-Ben; Deng, Xian-Qing; Song, Ming-Xia; 等.

LETTERS IN DRUG DESIGN & DISCOVERY  卷: 9   期: 4   页: 409-414   出版年: MAY 2012

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5楼2014-09-20 12:09:48
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