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Xian-Qing Deng, Chun-Rui Xiao, Cheng-Xi Wei, Zhe-Shan Quan. Synthesis and Anticonvulsant Activity of 5-Substituted-[1,2,4]triazolo[4,3-a]quinazolines. CHINESE J ORG CHEM, 2011, 31(12):2082.
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感谢参与,应助指数 +1
dengxianqing: 金币+3, ★★★★★最佳答案 2014-09-20 12:41:15
oven1986: LS-EPI+1, 感谢应助! 2014-09-21 00:37:11
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dengxianqing: 金币+2 2014-09-20 12:41:40
Synthesis and Anticonvulsant Activity of 5-Substituted-[1,2,4]triazolo[4,3-a]quinazolines


作者eng, XQ (Deng Xianqing)[ 1 ] ; Xiao, CR (Xiao Chunrui)[ 1 ] ; Wei, CX (Wei Chengxi)[ 1 ] ; Quan, ZS (Quan Zheshan)[ 1 ]




CHINESE JOURNAL OF ORGANIC CHEMISTRY



卷: 31

期: 12

页: 2082-2087

出版年: DEC 2011

查看期刊信息





























摘要

A series of 5-substituted-[1,2,4]triazolo[4,3-a]quinazolines were synthesized. The anticonvulsant effects and neurotoxicity of the compounds were evaluated with maximal electroshock test and rotarod test with intraperitoneally injected in mice. The pharmacology results showed that 5-pentyloxy-[1,2,4]triazolo[4,3-a]quinazoline (2d) was the most potent with ED50 value of 19.7 mg/kg and protective index (PI=TD50/ED50) value of 6.2. To explain the possible mechanism of anticonvulsant activity, compound 2d was tested in several chemical induced seizures tests. The results revealed that compound 2d was effective against the seizures induced by pentylenetetrazole, isoniazid, 3-mercaptopropionic acid and thiosemicarbazide, which suggested that the anticonvulsant effects of this series compounds were acted via increasing gamma-aminobutyric acid (GABA) ergic neurotransmission and activating glutamate decarboxylase (GAD) or inhibiting a-oxoglutarate aminotransferase (GABA-T) in the brain.


关键词

作者关键词:triazoloquinazoline; synthesis; anticonvulsant; pentylenetetrazole; rotarod test

KeyWords Plus:ANTIEPILEPTIC DRUGS; SEIZURES; EPILEPSY; GABA


作者信息

通讯作者地址: Deng, XQ (通讯作者)





Yanbian Univ, Coll Pharm, Yanji 133002, Peoples R China.





地址:





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





电子邮件地址:zsquan@ybu.edu.cn


出版商

SCIENCE PRESS, 16 DONGHUANGCHENGGEN NORTH ST, BEIJING 100717, PEOPLES R CHINA


类别 / 分类

研究方向:Chemistry

Web of Science 类别:Chemistry, Organic


文献信息

文献类型:Article

语种:Chinese

入藏号: WOS:000299064500013

ISSN: 0253-2786


期刊信息


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


其他信息

IDS 号: 875VY

Web of Science 核心合集中的 "引用的参考文献": 17

Web of Science 核心合集中的 "被引频次": 3
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dengxianqing: 金币+3, ★★★很有帮助 2014-09-20 12:41:45
入藏号: WOS:000299064500013
4楼2014-09-20 11:59:55
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被引频次: 3
https://apps.webofknowledge.com/ ... FromNonInterProduct






1.






Synthesis and In vitro Anticancer Activity of Novel Quinazoline Derivatives Containing Thiosemicarbazone Structure

作者: Liu Haibin; Lu Ping; Pan Ningning; 等.

CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE  卷: 35   期: 5   页: 981-988   出版年: MAY 2014

出版商处的全文



查看摘要

被引频次: 0
(来自 Web of Science 的核心合集)






2.






Regioselective Multi-component Synthesis of 7-Aryl-benzo[h][1,2,4]-triazolo[5,1-b]quinazoline-5,6-diones Catalyzed by n-Propylsulfonated gamma-Al2O3

作者: Li, Weilin; Tian, Shuanbao; Wu, Liqiang

BULLETIN OF THE KOREAN CHEMICAL SOCIETY  卷: 34   期: 9   页: 2825-2828   出版年: SEP 20 2013

出版商处的全文





被引频次: 0
(来自 Web of Science 的核心合集)






3.






Synthesis and Fungicidal Activity of 1,2,4-Triazole Derivatives Containing 2-Fluorophenyl Moiety

作者: Tong Jianying; Shi Yanxia; Liu Xinghai; 等.

CHINESE JOURNAL OF ORGANIC CHEMISTRY  卷: 32   期: 12   页: 2373-2377   出版年: DEC 2012

出版商处的全文



查看摘要
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