手性包公藤甲素类似物的制备及其生物活性

THE PREPARATION AND BIOACTIVITIES OF CHIRAL ANALOGS OF BAOGONGTENG A

用化学拆分技术制备了８个手性包公藤甲素类似物，经兔眼缩瞳或扩瞳试验表明，其中（－）３α对甲苯磺酰氧基６β乙酰氧基莨菪烷有拟胆碱作用。

Eight chiral analogs of baogongteng A were prepared from (±) 3α hydroxy 6β acetoxytropane by chemical resolution. In myotic or mydriatic tests in rabbits, (-) 3α paramethyl benzenesulfonyloxy 6β acetoxytropane showed cholinergic activities, while (+) 3α benzoyloxy 6β acetoxytropane and (+) 3α parachloro benzoyloxy 6β acetoxytropane showed anticholinergic activities.