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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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Synthesis and Anticonvulsant Activity of 5-Substituted-[1,2,4]triazolo[4,3-a]quinazolines


×÷Õßeng, XQ (Deng Xianqing)[ 1 ] ; Xiao, CR (Xiao Chunrui)[ 1 ] ; Wei, CX (Wei Chengxi)[ 1 ] ; Quan, ZS (Quan Zheshan)[ 1 ]




CHINESE JOURNAL OF ORGANIC CHEMISTRY



¾í: 31

ÆÚ: 12

Ò³: 2082-2087

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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.


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×÷Õ߹ؼü´Ê:triazoloquinazoline; synthesis; anticonvulsant; pentylenetetrazole; rotarod test

KeyWords Plus:ANTIEPILEPTIC DRUGS; SEIZURES; EPILEPSY; GABA


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ͨѶ×÷ÕßµØÖ·: Deng, XQ (ͨѶ×÷Õß)





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





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





µç×ÓÓʼþµØÖ·:zsquan@ybu.edu.cn


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


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Ñо¿·½Ïò:Chemistry

Web of Science Àà±ð:Chemistry, Organic


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ÎÄÏ×ÀàÐÍ:Article

ÓïÖÖ:Chinese

Èë²ØºÅ: WOS:000299064500013

ISSN: 0253-2786


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Impact Factor (Ó°ÏìÒò×Ó): Journal Citation Reports®


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