某些5-烷氧基-3H-1,4-苯并二氮杂卓-2(1H)-酮的合成及中枢神经系统评价
Synthesis and central nervous system evaluation of some 5-alkoxy-3H-1,4-benzodiazepin-2(1H)-ones.
作者信息
Gogerty J H, Griot R G, Habeck D, Iorio L C, Houlihan W J
出版信息
J Med Chem. 1977 Jul;20(7):952-6. doi: 10.1021/jm00217a019.
PMID:874970
Abstract
A series of 1-R-5-alkoxy-3H-1,4-benzodiazepin-2(1H)-ones was prepared and evaluated for central nervous system depressant activity. Several of these compounds, in particular, 7-chloro-5-ethoxy-1-methyl-3H-1,4-benzodiazepin-2(1H)-one (2), gave a profile and activity level similar to diazepam when measured in mice.
摘要
制备了一系列1-R-5-烷氧基-3H-1,4-苯并二氮杂䓬-2(1H)-酮，并对其进行中枢神经系统抑制活性评估。其中几种化合物，特别是7-氯-5-乙氧基-1-甲基-3H-1,4-苯并二氮杂䓬-2(1H)-酮（2），在小鼠实验中测得的作用特征和活性水平与地西泮相似。
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