作者:Michael R. Pavia、Charles P. Taylor、Fred M. Hershenson、Sandra J. Lobbestael
DOI:10.1021/jm00390a015
日期:1987.7
The anticonvulsant effect of a series of 6-alkoxy-N,N-disubstituted-2-pyridinamines is described. An investigation was carried out to optimize the activity/side-effect ratio in this series of compounds. The most desirable profile was seen with 1-[6-(2-methylpropoxy)-2-pyridinyl]piperazine, 6, and this compound was selected for a more complete pharmacological evaluation. Overall, 6 has a pharmacological
描述了一系列6-烷氧基-N,N-二取代-2-吡啶胺的抗惊厥作用。进行了研究以优化该系列化合物中的活性/副作用比。用1- [6-(2-(2-甲基丙氧基)-2-吡啶基]哌嗪6]观察到最理想的特性,选择该化合物进行更完整的药理评估。总体而言,6的药理特性与二苯乙内酰脲(苯妥英)非常相似。虽然与苯妥英几乎等效,但动物研究表明作用时间相当短。此外,有6例表现出一些麻烦的副作用,包括中枢神经系统抑制和体温过低。