.7 - Substituted Phenoxy-4 ,5 - Dihydro-1 ,2,4 - Triazolo [4,3-a] Quinoline And Quinoline -1 (2h) - One Derivatives And Anticonvulsant Activity

A series of 7-substituted-phenoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-α]quinolines and 7-substituted-phenoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-α]quinoline-1(2H)-ones was synthesized. And the compound the convulsanteffect and neurotoxicity were calculated with maximal electroshock test(MES), pentylenetetrazol (PTZ) and rotarod test via intraperitoneally inmice. The compound 7-(4-fluoro-phenyloxy)-4,5-dihydro-[1,2,4] triazolo[4,3-α]quinoline-1(2H)-one (3c) was among the most active but also hasthe lowest toxicity. In the anti-MES potency test, it showed medianeffective dose (ED₅₀) of 6.8 mg/kg, median toxicity dose (TD₅₀) of 88.0mg/kg, and the protective index (PI) of 12.9. The PI value of compound3c was better than that of marketed drugs phenytoin.