2-苯并氮杂䓬。2. 噻唑并[5,4-d][2]苯并氮杂䓬。

2-Benzazepines. 2. Thiazolo[5,4-d][2]benzazepines.

作者信息

Benjamin L E, Fryer R I, Gilman N W, Trybulski E J

出版信息

J Med Chem. 1983 Jan;26(1):100-3. doi: 10.1021/jm00355a020.

Abstract

As part of a program in the area of annelated 2-benzazepines, several thiazolo[5,4-d))[2]benzazepines were prepared. Treatment of the bromo ketones 7-9 with various thio amides gave the thiazoles 10-15, which when treated with methylamine gave the title compounds. The preliminary pharmacology of these compounds showed that they had central nervous system activity similar to the 1,4-benzodiazepines, such as diazepam. The thiazolo[5,4-d][2]benzazepines were also found to bind to the benzodiazepine-receptor complex, indicating that their pharmacological actions are probably related to the 1,4-benzodiazepines.

摘要

作为稠合2-苯并氮杂䓬领域项目的一部分，制备了几种噻唑并[5,4 - d][2]苯并氮杂䓬。用各种硫代酰胺处理溴代酮7 - 9得到噻唑10 - 15，噻唑10 - 15再用甲胺处理得到目标化合物。这些化合物的初步药理学研究表明，它们具有与1,4 - 苯二氮䓬类药物（如地西泮）相似的中枢神经系统活性。还发现噻唑并[5,4 - d][2]苯并氮杂䓬能与苯二氮䓬受体复合物结合，这表明它们的药理作用可能与1,4 - 苯二氮䓬类药物有关。