阿托品、东莨菪碱和托品酰胺具有广泛的抗胆碱作用,在眼科治疗中可用作扩瞳剂和睫状肌麻痹剂,但常出现伴有全身性副作用。为了减少副作用,本文作者将软药概念用于东莨菪碱/甲基东莨菪碱中,假设甲基东莨菪碱(Ⅰ)的伯醇在代谢过程中转化为羧酸(Ⅱ),并以此作为先导化合物,将其中的羧基用直链或环状烃基(R)酯化,设计合成了6个软性抗胆碱药(3a～f)。在豚鼠回肠中测定这些化合物抗胆碱作用 Atropine, scopolamine and tropicamide have a wide range of anticholinergic properties and are useful as mydriatic and cycloplegic agents in ophthalmic therapy, but often with systemic side effects. In order to reduce the side effects, the authors apply the concept of soft drug to scopolamine / methylscopolamine. Assuming that the primary alcohol of scopolamine (I) is converted to carboxylic acid (II) during the metabolic process, as the lead compound, Of the carboxyl group with a linear or cyclic hydrocarbon (R) esterification, design and synthesis of six soft anticholinergics (3a ~ f). The anticholinergic effects of these compounds were determined in guinea pig ileum