He H M, Shen J X, Ma X Y, He X P
Yao Xue Xue Bao. 1989;24(5):335-40.
The C2 deoxy and C6 electron isosteric analogs of a new antiglaucoma agent, erycibe alkaloid II, were designed and synthesized. The main pharmacological results were as follows: 1. The C2-OH in erycibe alkaloid II was one of the key groups for its myotic activity; 2. It was worth noting that compounds 2 and 4 showed cholinergic and anticholinergic activities, respectively. This phenomenon in tropane alkaloids was not reported before; 3. The C6 electron isosteric compounds 16 and 17 showed neither anticholinergic nor cholinergic activities.
设计并合成了一种新型抗青光眼药物刺桐生物碱II的C2脱氧和C6电子等排体类似物。主要药理结果如下：1. 刺桐生物碱II中的C2-OH是其缩瞳活性的关键基团之一；2. 值得注意的是，化合物2和4分别表现出胆碱能和抗胆碱能活性。这种在托烷生物碱中的现象此前未见报道；3. C6电子等排体化合物16和17既不表现出抗胆碱能活性也不表现出胆碱能活性。
