Synthesis and evaluation of heterobivalent tacrine derivatives as potential multi-functional anti-Alzheimer agents

…, YP Li, Y He, SL Huang, D Li, LQ Gu, ZS Huang

Index: Luo, Wen; Li, Yan-Ping; He, Yan; Huang, Shi-Liang; Li, Ding; Gu, Lian-Quan; Huang, Zhi-Shu European Journal of Medicinal Chemistry, 2011 , vol. 46, # 6 p. 2609 - 2616

Full Text: HTML

Citation Number: 39

Abstract

Abstract A new series of heterobivalent tacrine derivatives were designed, synthesized and evaluated as potential multi-functional anti-Alzheimer agents for their inhibitory activity on cholinesterases, antioxidant activity and self-induced β-amyloid (Aβ) aggregation. All these synthesized compounds had potent inhibition activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) at nanomolar range. A Lineweaver–Burk plot and ...