Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives
作者:Yasuo Oshiro、Youji Sakurai、Tatsuyoshi Tanaka、Tetsuro Kikuchi、Tsuyoshi Hirose、Katsura Tottori
DOI:10.1021/jm00111a014
日期:1991.7
In a continuous search for a novel cerebroprotective drug with a central nervous system (CNS) stimulating activity, a series of 1-(acylamino)-7-hydroxyindan derivatives has been synthesized and tested for its dual activities. The cerebroprotective activities of the compounds in this series were evaluated in terms of their effect on the survival of mice in hypoxic conditions (210 mmHg), and their CNS
在不断寻找具有中枢神经系统(CNS)刺激活性的新型脑保护药物时,已合成了一系列1-(酰基氨基)-7-羟基茚满衍生物,并对其双重活性进行了测试。根据其对低氧条件下(210 mmHg)小鼠存活的影响,评估了该系列化合物的脑保护活性,并通过评估其对脑震荡引起的昏迷恢复的促进作用,检查了其对中枢神经系统的刺激活性。在小鼠中。几种化合物以30 mg / kg po的剂量延长了低氧条件下小鼠的存活率。该系列中的四种化合物在相同剂量下均表现出CNS刺激作用。其中,7-羟基-1-[[4-(3-甲氧基苯基)-1-哌嗪基]乙酰基]氨基] -2,2,4,6-四甲基茚满(18,OPC-14117),