College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, PR China.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1532-4. doi: 10.1016/j.bmcl.2010.01.097. Epub 2010 Jan 25.
A series of physostigmine analogues were prepared and evaluated for cholinesterase inhibition activities, including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of them showed potent inhibition activities against AChE, in which compound 17 especially exhibited significantly higher selectivity over BChE than phenserine, a compound currently on clinical trial. Discussion about the relationships between structure and activity of these derivatives was also presented.
一系列毒蕈堿类似物被制备并评估了其对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）的抑制活性。它们大多数对 AChE 具有很强的抑制活性，其中化合物 17 对 BChE 的选择性明显高于正在临床试验中的化合物苯甲曲秦。还讨论了这些衍生物的结构与活性之间的关系。
