Abstract

The synthesis of four tetra-tacrine clusters where the tacrine binding units are attached to a central scaffold via linkers of variable lengths is described. The multivalent inhibition potencies for the tacrine clusters were investigated for the inhibition of acetylcholinesterase. Two of the tacrine clusters displayed a small but significant multivalent inhibition potency in which the binding affinity of each of the tacrine binding units increased up to 3.2 times when they are connected to the central scaffold.

中文翻译：

---

开发他克林簇作为抑制乙酰胆碱酯酶的正协同系统

摘要

描述了四个四他克林簇的合成，其中他克林结合单位通过可变长度的接头连接到中央支架上。研究了他克林簇的多价抑制效力以抑制乙酰胆碱酯酶。两个他克林簇显示出很小但显着的多价抑制效力，其中每个他克林结合单位的结合亲和力在它们连接到中央支架时增加了 3.2 倍。