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7-取代苯氧基－4, 5-二氢－1, 2, 4-三唑并[4, 3-a]喹啉和喹啉－1(2H)-酮衍生物的合成及抗惊厥活性

金云哲、关丽萍、赵立明、朴虎日、全哲山

2007Chemistry被引 0

摘要

A series of 7-(substituted phenoxyl)-4,5-dihydro-[1,2,4]thazolo4,3-a1qujnoljnes and 7-(substituted phenoxyl)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline-1(2H)-ones were synthesized. The convulsant effect and neurotoxicity of the compound were determined with maximal electroshock test (MES), pentylenetetrazol (PTZ) method and rotarod test intraperitoneally in mice. 7-(4-Fluorophenyloxy)-4,5-dihydro-[l,2,4]triazolo[4,3-a]quinoljne-1(2H)-one (4c) was the most active and also has the lowest toxicity. In the anti-MES potency test, 4c showed a medial effective dose (ED50) of 6.8mg/kg, a medial toxicity dose (TD) of 88.0mg/kg, and the protective index (PI) of 12.9. The PI value of compound 4c was better than that of the marketed drug phenytoin.

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