Design, synthesis and pharmacological evaluation of novel tacrine–caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease

…, Z Cheng, P Liu, Y Wang, J Yu, Y Tan, Y Huang…

Index: Chao, Xiaojuan; He, Xixin; Yang, Yilin; Zhou, Xie; Jin, Minghua; Liu, Shu; Cheng, Zhiyi; Liu, Peiqing; Wang, Yuting; Yu, Jianchen; Tan, Yi; Huang, Yingjuan; Qin, Jian; Rapposelli, Simona; Pi, Rongbiao Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 20 p. 6498 - 6502

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Citation Number: 43

Abstract

A novel series of tacrine–caffeic acid hybrids (5a–f) were designed and synthesized by combining caffeic acid (CA) with tacrine. The antioxidant study revealed that all the hybrids have much more antioxidant capacities compared to CA. Among these compounds, 5e showed the highest selectivity in inhibiting acetylcholinesterase (AChE) over butyrylcholinesterase (BuChE). Enzyme kinetic study had suggested that 5e binds to both ...