Brewer M D, Burgess M N, Dorgan R J, Elliott R L, Mamalis P, Manger B R, Webster R A
Beecham Pharmaceuticals Research Division, Tadworth, Surrey, England.
J Med Chem. 1989 Sep;32(9):2058-62. doi: 10.1021/jm00129a007.
A series of 1,2,3,4,6,7,8,12b-octahydropyrazino[2,1-alpha][2] benzazepine derivatives was prepared and the cestocidal activity of the compounds evaluated in an in vitro Taenia crassiceps screen. Many of these derivatives proved to be highly active, and 2-(cyclohexylcarbonyl)-4-oxo-1,2,3,4,6,7,8,12b- octahydropyrazino[2,1-alpha][2]benzazepine, epsiprantel (BAN) (22), was selected for further development. The structure-activity relationships are discussed.
制备了一系列1,2,3,4,6,7,8,12b-八氢吡嗪并[2,1-α][2]苯并氮杂䓬衍生物，并在体外筛选克氏带绦虫的实验中评估了这些化合物的杀绦虫活性。事实证明，其中许多衍生物具有很高的活性，2-(环己基羰基)-4-氧代-1,2,3,4,6,7,8,12b-八氢吡嗪并[2,1-α][2]苯并氮杂䓬，即埃普瑞奈（BAN）（22），被选中作进一步研发。文中讨论了构效关系。
