2-苯并氮杂䓬。4. [1,2,3]三唑并[4,5-d][2]苯并氮杂䓬和二苯并[c,f][1,2,3]三唑并[3,4-a]氮杂䓬：作为中枢神经系统药物的合成与评价
2-Benzazepines. 4. [1,2,3]Triazolo[4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines: synthesis and evaluation as central nervous system agents.
作者信息
Trybulski E J, Benjamin L, Vitone S, Walser A, Fryer R I
出版信息
J Med Chem. 1983 Mar;26(3):367-72. doi: 10.1021/jm00357a011.
The facile synthesis of [1,2,3]triazolo((4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines by the addition of sodium azide to acetylenic benzophenones is described. Examination of the pharmacological data indicates that selected triazolobenzazepines are as potent as diazepam in the anti-pentylenetetrazole test and are weaker in the inclined screen and rotarod tests, suggesting that these compounds have antianxiety properties similar to diazepam with fewer deficits in motor coordination. In addition, a possible diazepam antagonist was found in the triazolo-benzazepine series. The dibenzotriazoloazepines were found to be inactive in four standard CNS screening procedures.
描述了通过向炔基二苯甲酮中加入叠氮化钠轻松合成[1,2,3]三唑并((4,5 - d][2]苯并氮杂卓和二苯并[c,f][1,2,3]三唑并[3,4 - a]氮杂卓的方法。对药理数据的研究表明，所选的三唑并苯并氮杂卓在抗戊四氮试验中与地西泮效力相当，而在倾斜屏幕试验和旋转棒试验中效力较弱，这表明这些化合物具有与地西泮相似的抗焦虑特性，且运动协调性缺陷较少。此外，在三唑并苯并氮杂卓系列中发现了一种可能的地西泮拮抗剂。发现二苯并三唑并氮杂卓在四种标准的中枢神经系统筛选程序中无活性。
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