Ellefson C R, Woo C M, Miller A, Kehr J R
J Med Chem. 1978 Sep;21(9):952-7. doi: 10.1021/jm00207a020.
2-Amino-4-aryl-3H-1,5-benzodiazepines were prepared and evaluated for potential neuroleptic activity. Compound 60 showed some activity in the four assays; however, the activity was not consistently observed among other members of the series. The data reflected that the structural modifications led to a decrease in activity relative to clozapine. It was apparent that the 1,5-benzodiazepine portion of clozapine is not responsible for its antipsychotic activity.
制备了2-氨基-4-芳基-3H-1,5-苯二氮䓬类化合物，并对其潜在的抗精神病活性进行了评估。化合物60在四项试验中表现出一定活性；然而，该系列的其他成员并未始终观察到这种活性。数据表明，相对于氯氮平，结构修饰导致活性降低。显然，氯氮平的1,5-苯二氮䓬部分与其抗精神病活性无关。
