Synthesis and Studies on the Anticonvulsant Activity of 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine Derivatives
作者:L.-P. Guan、R.-P. Zhang、Y. Sun、Y. Chang、X. Sui
DOI:10.1055/s-0032-1314821
日期:2012.8
In this study, a series of new 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine derivatives was synthesized and their anticonvulsant activity and neurotoxicity was evaluated with the maximal electroshock and rotarod tests, respectively. The most promising compounds, 3p (5-(4-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridine) and 3r (5-(4-bromophenoxy)-[1,2,4]triazolo[4,3-a]pyridine), showed a median effective dose
在这项研究中,合成了一系列新的5-烷氧基-[1,2,4]三唑并[4,3-a]吡啶衍生物,并分别通过最大电击和旋转脚踏试验测试了它们的抗惊厥活性和神经毒性。最有前途的化合物3p(5-(4-氯苯氧基)-[1,2,4]三唑并[4,3-a]吡啶)和3r(5-(4-溴苯氧基)-[1,2,4]三唑并[4,3-a]吡啶)的平均有效剂量为13.2和15.8 mg / kg,保护指数分别为4.8和6.9。为了探索推测的作用机理,在化学诱导模型中测试了化合物3n,3p和3r。