作者:Judith A. Clark、Michael S. G. Clark、Derek V. Gardner、Laramie M. Gaster、Michael S. Hadley、David Miller、Anwer Shah
DOI:10.1021/jm00197a018
日期:1979.11
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,