Synthesis and anticonvulsant activity evaluation of 8-alkoxy-5-(4H-1,2,4-triazol-4-yl)quinoline derivatives

다국어 초록 (Multilingual Abstract)

Two series of 8-alkoxy-5-(4H-1,2,4-triazol-4-yl)quinolines and 8-alkoxy-5-(2H-1,2,4-triazol-3-one-4-yl)quinolineswere synthesized.The anticonvulsant activity ofthese compounds was evaluated with maximal electroshockseizure test and rotarod test. Among the synthesized compounds,8-octoxy-5-(4H-1,2,4-triazol-4-yl)quinoline (4g)was the most active compound with ED50 of 8.80 mg/kg,TD50 of 176.03 mg/kg and protective index of 20.0. Itsneurotoxicity was lower than all other synthesized compoundsand also markedly lower than that of the referencedrug carbamazepine. In addition, the potency of compound 4gagainst seizures induced by pentylenetetrazole, 3-mercaptopropionicacid, and bicuculline suggested its broad spectrumactivity, and the mechanisms of action including inhibition ofvoltage-gated ion channels and modulation of GABAergicactivity might involve in its anticonvulsant activity.

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