Fryer R I, Leimgruber W, Trybulski E J
J Med Chem. 1982 Sep;25(9):1050-5. doi: 10.1021/jm00351a009.
The syntheses of 2-amino-N-(2-benzoyl)-4-chlorophenyl)acetamides are reported. The pharmacological properties of these compounds were compared with data obtained from the corresponding cyclized products [5-(2,6-dichlorophenyl)-1,4-benzodiazepin-2-ones]. Evidence is presented which suggests that the central nervous system activity observed for 1,4-benzodiazepines is inherent only in the closed seven-membered ring and is not due to the ring-opened form.
报道了2-氨基-N-(2-苯甲酰基)-4-氯苯基)乙酰胺的合成。将这些化合物的药理性质与从相应的环化产物[5-(2,6-二氯苯基)-1,4-苯并二氮杂卓-2-酮]获得的数据进行了比较。所提供的证据表明，观察到的1,4-苯并二氮杂卓的中枢神经系统活性仅存在于封闭的七元环中，而非开环形式。
