Stout D M, Gorczynski R J
J Med Chem. 1982 Mar;25(3):326-8. doi: 10.1021/jm00345a019.
Seven derivatives of 2-[[2-(3,4-dihydroxyphenyl)-1-methylethyl]amino]-6,7-dihydroxy-1,2,3,4- tetrahydronaphthalene, an inotropic agent which also causes a decrease in blood pressure, were synthesized and tested for inotropic potency, cardioselectivity, and inotropic selectivity. The derivatives were designed to explore whether catechol moieties and rigid rotamers of dopamine are necessary for the activity which was found in the parent compound. The derivatives had phenolic functions in place of catechols, and they had phenethylamine in place of the tetrahydronaphthalene moiety. In no case was the profile of activity of the parent compound duplicated in the derivatives.
合成了2-[[2-(3,4-二羟基苯基)-1-甲基乙基]氨基]-6,7-二羟基-1,2,3,4-四氢萘的七种衍生物，该正性肌力药也会导致血压下降，并对其正性肌力效能、心脏选择性和正性肌力选择性进行了测试。设计这些衍生物是为了探究儿茶酚部分和多巴胺的刚性旋转异构体对于母体化合物中发现的活性是否必要。这些衍生物具有酚羟基官能团来取代儿茶酚，并且用苯乙胺取代了四氢萘部分。在任何情况下，衍生物都没有重现母体化合物的活性特征。
