discovery that 3-(dimethylamino)-1,1-diphenyl-2-propanol hydrobromide (1) possesses potent reserpine-prevention activity in mice, a series of analogues of 1 was synthesized and evaluated as potential antidepressant agents. Several routes to analogues of 1 were evaluated, the most generally applicable of which was the regiospecific ring opening of a suitably functionalized 1,1-diaryl-2,3-epoxypropane (obtained
在发现3-(二甲基
氨基)-
1,1-二苯基-2-丙醇氢溴酸盐(1)在小鼠中具有有效的
利血平预防活性后,合成了一系列类似物1,并被评估为潜在的抗抑郁药。评价了几种类似物1的途径,其中最普遍适用的是用适当的胺将适当官能化的1,1-二芳基-2,3-环氧
丙烷(从相应的
二苯甲酮分三个阶段获得)的区域特异性开环。评价了该系列中更有趣的化合物引起不期望的外周抗
胆碱能作用的倾向,所有测试的化合物在该参数上的活性均明显低于
丙咪嗪。基于其在抑郁症的生化和药理动物模型中的良好活性,