DeWald H A, Lobbestael S, Butler D E
J Med Chem. 1977 Dec;20(12):1562-9. doi: 10.1021/jm00222a005.
A series of 4-aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e] [1,4]diazepin-7(1H)-ones was synthesized and screened for psychotropic activity. In animals, a number of these pyrazolodiazepinones had strong CNS effects similar to diazepam. One compound, 4-(2-fluorophenyl)-6,8-dihydro-1,3,8-trimethylpyrazolo[3,4-e] [1,4]diazepin-7(1H)-one (54), is being studied in the clinic as a component of a new animal anesthetic, Tilazol.
合成了一系列4-芳基-1,3-二烷基-6,8-二氢吡唑并[3,4-e][1,4]二氮杂卓-7(1H)-酮,并对其精神活性进行了筛选。在动物实验中,许多这类吡唑并二氮杂卓酮具有与地西泮相似的强烈中枢神经系统作用。一种化合物,4-(2-氟苯基)-6,8-二氢-1,3,8-三甲基吡唑并[3,4-e][1,4]二氮杂卓-7(1H)-酮(54),正在作为一种新型动物麻醉剂Tilazol的成分进行临床研究。