A series of phenacyl triazole hydrazones 3 have been designed based on the hybridization of (arylalkly)triazole and aroyl hydrazone scaffolds as new anticonvulsant agents. The target compounds 3 were easily synthesized from appropriate phenacyl triazoles and aryl acid hydrazides and characterized by IR, NMR and Mass spectroscopy. The in vivo anticonvulsant evaluation of synthesized compounds by using MES and PTZ tests revealed that they are more effective in MES model respect to PTZ test. All compounds showed 33–100% protection against MES-induced seizures at the dose of 100 mg/kg. However, the isonicotinic acid hydrazide derivative 3h showed the best profile of activity in both models. Molecular docking studies of compound 3h with different targets (NMDA, AMPA, GABA_A and sodium channel), postulated that the compound acts mainly via GABA_A receptors. In silico molecular properties predictions indicated that all compounds have favourable oral bioavailability and BBB permeability.

基于（芳基烷基）三唑和芳酰基hydr支架作为新的抗惊厥剂的杂交，设计了一系列的苯甲酰基三唑3。由适当的苯甲酰基三唑和芳基酰肼容易地合成目标化合物3，并通过IR，NMR和质谱进行表征。通过使用MES和PTZ测试对合成化合物进行体内抗惊厥评估，发现它们在MES模型方面相对于PTZ测试更有效。在100 mg / kg的剂量下，所有化合物对MES引起的癫痫发作均显示出33-100％的保护作用。但是，异烟酸酰肼衍生物3h在两个模型中均显示出最佳的活性曲线。化合物3h的分子对接研究具有不同靶标（NMDA，AMPA，GABA _A和钠通道）的化合物，假定该化合物主要通过GABA _A受体起作用。在计算机上的分子特性预测表明，所有化合物均具有良好的口服生物利用度和BBB渗透性。