Hester J B, Von Voigtlander P
J Med Chem. 1979 Nov;22(11):1390-8. doi: 10.1021/jm00197a021.
A series of 1-substituted 6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines was prepared and evaluated for central nervous system activity. It was found that electronegative substituents, such as trifluoromethyl, were detrimental to activity in this series. On the other hand, many compounds with electron-donating substituents at C-1 had interesting activity. In addition to showing anxiolytic potential, some were also active in tests useful for detecting antidepressant and antipsychotic activity. Several analogues with 4-methyl-1-piperazinyl and 4-morpholinyl substituents at C-1 were of particular interest.
制备了一系列1-取代的6-芳基-4H-1,2,4-三唑并[4,3-a][1,4]苯二氮䓬类化合物，并对其进行了中枢神经系统活性评估。结果发现，吸电子取代基，如三氟甲基，对该系列化合物的活性不利。另一方面，许多在C-1位带有供电子取代基的化合物具有有趣的活性。除了显示出抗焦虑潜力外，一些化合物在用于检测抗抑郁和抗精神病活性的试验中也具有活性。几种在C-1位带有4-甲基-1-哌嗪基和4-吗啉基取代基的类似物尤其令人关注。
