The new series of N-(5,6-diphenyl-1,2,4-triazin-3-yl)-2-(4-substituted piperazin-1-yl) acetamide (RP1–5) and 2-((5,6-diphenyl-1,2,4-triazin-3-yl)thio)-1-(4- substituted piperazin-1-yl)-ethan-1-one (RP6–10) derivatives were designed and synthesised by clubbing substituted 5,6-diphenyl-1,2,4-triazine with different substituted piperazines. The synthesized compounds were tested for anticonvulsant activity and various biochemical toxicity parameters. Among the series, two compounds (2-(4-benzylpiperazin-1-yl)-N-(5,6-diphenyl-1,2,4-triazin-3-yl)acetamide (RP4), and 2‑chloro-1-(4-substituted piperazin-1-yl)ethan-1-one (RP5) were found to demonstrate the most potent anticonvulsant activity in both MES and scPTZ convulsion mice models. The most active compound RP5 was effective at median doses (ED₅₀) of 14.82 mg/kg in MES and 14.61 mg/kg in scPTZ model. The median toxic dose (TD₅₀) was > 600 which provided the compound RP5 with high protective index of 40.48 in the MES test and 41.06 in scPTZ test. Further, both the compounds were also found to possess significant antidepressant activity. The compounds did not show any adverse effect in various parameters such as grip-strength test (skeletal muscular strength), actophotometer, and rotarod test (locomotor) as compared to the control groups. In biochemical estimation, RP4 and RP5 were found nontoxic and showed no sign of any pathological changes in blood chemistry, liver, and nephrology of the kidney. The GABA level estimation in the whole brain of mice was performed to predict the mechanistic study of the selected compounds.

新系列N-(5,6-diphenyl-1,2,4-triazin-3-yl)-2-(4-取代哌嗪-1-yl)乙酰胺(RP1-5)和2-((5 ,6-diphenyl-1,2,4-triazin-3-yl)thio)-1-(4-取代 piperazin-1-yl)-ethan-1-one (RP6-10) 衍生物通过棒棒状设计和合成用不同的取代哌嗪取代5,6-二苯基-1,2,4-三嗪。测试合成的化合物的抗惊厥活性和各种生化毒性参数。该系列中有两种化合物（2-(4-benzylpiperazin-1-yl)-N-(5,6-diphenyl-1,2,4-triazin-3-yl)acetamide (RP4) 和 2-chloro-发现 1-(4-取代的 piperazin-1-yl)ethan-1-one (RP5) 在 MES 和 scPTZ 惊厥小鼠模型中表现出最有效的抗惊厥活性。最活跃的化合物 RP5 在中等剂量 (ED ₅₀) 在 MES 中为 14.82 mg/kg，在 scPTZ 模型中为 14.61 mg/kg。中位毒性剂量(TD ₅₀ )>600，这使得化合物RP5在MES测试中具有40.48的高保护指数，在scPTZ测试中具有41.06的高保护指数。此外，还发现这两种化合物都具有显着的抗抑郁活性。与对照组相比，这些化合物在握力测试（骨骼肌力量）、光度计和旋转棒测试（运动）等各种参数中没有显示出任何不利影响。在生化评估中，发现 RP4 和 RP5 无毒，并且在血液化学、肝脏和肾脏的肾脏学方面没有任何病理变化的迹象。对小鼠全脑中的 GABA 水平进行了估计，以预测所选化合物的机理研究。