Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase

Journal of Enzyme Inhibition and Medicinal Chemistry

José G. Fernández-Bolaños¹  Óscar López¹  Emil Lindbäck²  Tereza Cristina Santos Evangelista²  Magne O. Sydnes²  Sabrina Baptista Ferreira³ 

[1] Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla;Department of Chemistry, Bioscience and Environmental Engineering, Faculty of Science and Technology, University of Stavanger;Department of Organic Chemistry, Chemistry Institute, Federal University of Rio de Janeiro;

关键词: acetylcholinesterase;    cuaac;    multivalent interactions;    multivalent inhibition potency;    tacrine;   

DOI  :  10.1080/14756366.2021.1954917

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown