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Synthesis and Anticonvulsant Activity of 5-substituted-[1,2,4] Triazolo [4,3-α] Quinazolines

Author: XiaoChunRui
Tutor: QuanZheShan
School: Yanbian University
Course: Medicinal Chemistry
Keywords: Triazole Quinazoline Anticonvulsant Maximum electro-convulsive Pentylenetetrazol Isoniazid Thiosemicarbazide 3 - mercaptopropionate
CLC: R96
Type: Master's thesis
Year: 2011
Downloads: 19
Quote: 0
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Abstract


Antiepileptic compounds in order to find a good activity to 2,4 - dichloro- quinazoline as a starting material , design and synthesis of a series of 5 - substituted - [1,2,4] triazolo [4,3-α] quinazoline derivatives (2a-2q). Using murine maximum electric convulsion test (MES), and their anticonvulsant activity was measured using a rotary Determination neurotoxicity . Pharmacological results show : 5 - pentyloxy - [ 1,2,4 ] triazolo [ 4,3- α ] quinolizin oxazoline (2d) , an ED50 of 19.7mg/kg protection index for PI = 6.2 (PI = TD50 / ED50) shows better anticonvulsant activity . In order to clarify the mechanism of the possible anticonvulsant , the compound 2d were Subcutaneous Pentylenetetrazol , isoniazid, 3 - mercaptopropionic acid induced seizures in experimental and thiosemicarbazide . The results show that the compound 2d can be effectively against Pentylenetetrazol , isoniazid , thiosemicarbazone and 3 - mercaptopropionic acid induced seizures . By inference, this series of compounds may be activated by acting on neurotransmitter GABA system glutamic acid decarboxylase (GAD) , or the inhibition of α-keto- glutaric acid aminotransferase (GABA-T) to exert anticonvulsant effect .

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