Synthesis and studies on the anticonvulsant activity of 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine derivatives.

Arzneimittel-Forschung-Drug Research Pub Date : 2012-08-01 Epub Date: 2012-07-10 DOI:10.1055/s-0032-1314821
L-P Guan, R-P Zhang, Y Sun, Y Chang, X Sui
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引用次数: 16

Abstract

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 of 13.2 and 15.8 mg/kg and had a protective index value of 4.8 and 6.9, respectively. For exploring the putative mechanism of action, compounds 3n, 3p and 3r were tested in chemically induced models.

5-烷氧基-[1,2,4]三唑[4,3-a]吡啶衍生物的合成及抗惊厥活性研究。
本研究合成了一系列新的5-烷氧基-[1,2,4]三唑[4,3-a]吡啶衍生物,并分别用最大电击试验和轮棒试验评价了它们的抗惊厥活性和神经毒性。最有希望的化合物3p(5-(4-氯苯氧基)-[1,2,4]三唑[4,3-a]吡啶)和3r(5-(4-溴苯氧基)-[1,2,4]三唑[4,3-a]吡啶)的中位有效剂量分别为13.2和15.8 mg/kg,保护指数分别为4.8和6.9。为了探索可能的作用机制,化合物3n, 3p和3r在化学诱导模型中进行了测试。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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