Synthesis and Studies on Anticonvulsant Activity of 8-Alkoxy-[1,2,4]triazolo[4,3-a]pyrazine
作者:Li-Ping Guan、Rui-Peng Zhang、Yue Chang、Xi-Xi Gan
DOI:10.14233/ajchem.2013.13703
日期:——
In this study, a series of new 8-alkoxy-[1,2,4]triazolo[4,3-a]pyrazine derivatives were synthesized and their anticonvulsant activity and neurotoxicity were evaluated by the maximal electroshock test and the rotarod test, respectively. The most promising compounds 3d (8-butoxy-[1,2,4]triazolo[4,3-a]pyrazine) and 3f (8-hexyloxy-[1,2,4]triazolo[4,3-a]pyrazine) showed a median effective dose of 44 and 35.3 mg/kg and had protective index value of 3.2 and 4.8, respectively. To explain the possible mechanism of anticonvulsant activity, all compounds were tested in chemical induced model in anti pentylenetetrazol test.
本研究合成了一系列新的 8-烷氧基-[1,2,4]三唑并[4,3-a]吡嗪衍生物,并分别通过最大电击试验和旋转体试验评估了它们的抗惊厥活性和神经毒性。最有希望的化合物 3d(8-丁氧基-[1,2,4]三唑并[4,3-a]吡嗪)和 3f(8-己氧基-[1,2,4]三唑并[4,3-a]吡嗪)的中位有效剂量分别为 44 毫克/千克和 35.3 毫克/千克,保护指数分别为 3.2 和 4.8。为了解释抗惊厥活性的可能机制,所有化合物都在化学诱导模型中进行了抗戊烯四唑试验。