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KMID : 0043320170400040435
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Archives of Pharmacal Research
2017 Volume.40 No. 4 p.435 ~ p.443
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Design, synthesis and evaluation of 5-substituted 1-H-tetrazoles as potent anticonvulsant agents
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Liao Ai Mei
Wang Tian Tian
Cai Bang Rong
Jin Yi
Cheon Seung-Hoon
Chun Chang-Ju
Wang Zeng Tao
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Abstract
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A series of 5-substituted 1-H-tetrazoles were designed and synthesized as potent anticonvulsant agents. Their preliminary anticonvulsant activities were evaluated using maximal electroshock and subcutaneous pentylenetetrazole (scPTZ) seizure tests. Neurotoxicity was determined using rotarod test. The results indicated that the compound 2j in scPTZ model exhibited the ED50 values of 83.3 mg/kg, superior to the standard drug ethosuximide with the maximum activity. In addition, compound 2k showed the most potent activity in MES model with ED50 value of 9.6 mg/kg and TD50 value of 189.5 mg/kg after intraperitoneal injection in mice, and displayed a high protective index (TD50/ED50) of 19.7 compared to reference antiepileptic drugs.
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KEYWORD
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Synthesis, 5-Substituted 1-H-tetrazoles, Anticonvulsant
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