Ding W G, Yang L M, Yu Y M
Department of Chemistry, Shanghai Second Medical University.
Yao Xue Xue Bao. 1993;28(4):302-6.
Ten analogs of baogongteng A, the natural cholinergic tropane alkaloid isolated from Erycibe obtusifolia Benth, were designed and synthesized. The tropane skeleton was kept unchanged, while the substituting groups on N and C3 were modified. In myotic experiments in rabbits 3-paramethyl benzoyloxy-6-acetoxy nortropane(4), 3-propionyloxy-6-acetoxy nortropane(5), and 3-isobutyryloxy-6-acetoxy nortropane(6) showed cholinergic activities.
设计并合成了从丁公藤中分离得到的天然胆碱能托烷生物碱包公藤甲素的10种类似物。托烷骨架保持不变，同时对N和C3位上的取代基进行了修饰。在兔缩瞳实验中，3-对甲基苯甲酰氧基-6-乙酰氧基去甲托烷（4）、3-丙酰氧基-6-乙酰氧基去甲托烷（5）和3-异丁酰氧基-6-乙酰氧基去甲托烷（6）表现出胆碱能活性。
