Synthesis Of Novel 8-alkylamino-5, 6-dihydro-4H-benzo[f][1,2,4]Triazolo[4,3-a]Azepines As Anticonvulsant Agents

We have synthesized a series of 7-alkylamino 1,3,4,5-benzazepin compounds and triazole derivatives, by the maximal electroshock seizure (MES) test and subcutaneous pentylenetetrazol (scPTZ) test method evaluate its antiepileptic activity. Their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox).The results of these tests demonstrated that 8-(heptyl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo [4,3-a][1]benzoazepines (10g) has the best activity in this series of materials, the maximum electric convulsion (MES) the ED50=19.0;while the 8-(heptyl)-5, 6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1] benzodiazepines (10g), it’s ED50 is 19.0 and protection index (PI) is 14.8 in MES test, respectively. These value were better than prototype antiepileptic drug Phenobarbital and Valproate. The possible structure activity relationship was discussed.In discussing the possible structure-activity relationship and mechanism of action, the compound 10g of Maximal electroshock test has good activity, its mechanism is to blocking the Na+ channel, to achieve the effect of anti-epileptic.