| Synthesis and anticonvulsant activity of 7-benzylamino-4,5-dihydro-［1,2,4］triazolo［4,3-a］quinolines |
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| 作者姓名： | Cui Xiangshu Guan Liping Li Hailan Piao Huri and Quan Zheshan |
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| 作者单位： | 1.Key Laboratory of Organic Functional Factors of the Changbai Mountain，Ministry of Education，Yanbian University，Yanji 133002，China;2.College of Basic Medicine，Yanbian University，Yanji 133000，China;3.College of Pharmacy，Yanbian University，Yanji 133000，China |
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| 摘 要： | A series of 7-substituted-benzylamino-4,5-dihydro-1,2,4]triazolo4,3-a]quinoline derivatives was synthesized and evaluated for their anticonvulsant activity.The subcutaneous pentylenetetrazole test(sc-PTZ)demonstrated that the most effective compound in controlling the sc-PTZ induced seizure was 7-(3-bromine-benzylamino)-4,5-dihydro-1,2,4]triazolo4,3-a]quinoline(4j)with an ED50 of 5.0 mg/kg and the PI of 20.7,which was also safer than the reference drugs.And the maximal electroshock test(MES)demonstrated that among these derivatives,7-(3-fluorobenzylamino)-4,5-dihydro-1,2,4]trizolo4,3-a]quinoline(4i),with an ED50 of 15.3 mg/kg and the PI of 7.2,was the safest in MES test.Furthermore,their neurotoxicities were measured by the rotarod neurotoxicity test,and the results showed that all derivatives possessed lower neurotoxicity.
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Synthesis and anticonvulsant activity of 7-benzylamino-4, 5-dihydro- [ 1, 2, 4] triazolo[ 4, 3-a] quinolines |
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| Cui Xiangshu,Guan Liping,Li Hailan,Piao Huri and Quan Zheshan.Synthesis and anticonvulsant activity of 7-benzylamino-4, 5-dihydro- [ 1, 2, 4] triazolo[ 4, 3-a] quinolines[J].Progress in Natural Science,2007,17(9):1104-1108. |
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| Authors: | Cui Xiangshu Guan Liping Li Hailan Piao Huri and Quan Zheshan |
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| Institution: | 1. Key Laboratory of Organic Functional Factors of the Changbai Mountain, Ministry of Education, Yanbian University, Yanji 133002, China; 2. College of Basic Medicine, Yanbian University, Yanji 133000, China; 3. College of Pharmacy, Yanbian University, Yanji 133000, China |
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| Abstract: | A series of 7-substituted-benzylamino-4,5-dihydro-1,2,4]triazolo4,3-a]quinoline derivatives was synthesized and evaluated for their anticonvulsant activity.The subcutaneous pentylenetetrazole test(sc-PTZ)demonstrated that the most effective compound in controlling the sc-PTZ induced seizure was 7-(3-bromine-benzylamino)-4,5-dihydro-1,2,4]triazolo4,3-a]quinoline(4j)with an ED50 of 5.0 mg/kg and the PI of 20.7,which was also safer than the reference drugs.And the maximal electroshock test(MES)demonstrated that among these derivatives,7-(3-fluorobenzylamino)-4,5-dihydro-1,2,4]trizolo4,3-a]quinoline(4i),with an ED50 of 15.3 mg/kg and the PI of 7.2,was the safest in MES test.Furthermore,their neurotoxicities were measured by the rotarod neurotoxicity test,and the results showed that all derivatives possessed lower neurotoxicity. |
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| Keywords: | quinoline triazole synthesis anticonvulsant epilepsia |
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