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KMID : 0043320090320010023
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Archives of Pharmacal Research
2009 Volume.32 No. 1 p.23 ~ p.31
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Synthesis of 2-Substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles as Potential Anticonvulsant Agents
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Quan Zhe Shan
Chai Geu-Yun
Jia Jing-Hao
Guan Li-Ping
Wei Cheng-Xi
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Abstract
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A series of 2-substituted-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazoles were synthesized. The anticonvulsant effect and neurotoxicity of the compounds (intraperitoneally) were evaluated with the maximal electroshock (MES) test, subcutaneous pentylenetetrazole (sc-PTZ), and rotarod tests in mice. 2-Phenyl- 6- (4H-1,2,4-triazol-4-yl)benzo[d]oxazole (3g) was the most active and also had the lowest toxicity. In the anti-MES potency test, it showed median effective dose (ED50) of 29.5 mg/kg, a median toxicity dose (TD50) of 285 mg/kg, and a protective index (PI) of 9.7, which is greater than the reference drug, carbamazepine, which has a PI of 6.4.
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KEYWORD
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Synthesis, Benzo[d]oxazole, Triazole, Anticonvulsant activity
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