| Literature DB >> 22981331 |
Xiaojuan Chao1, Xixin He, Yilin Yang, Xie Zhou, Minghua Jin, Shu Liu, Zhiyi Cheng, Peiqing Liu, Yuting Wang, Jianchen Yu, Yi Tan, Yingjuan Huang, Jian Qin, Simona Rapposelli, Rongbiao Pi.
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 catalytic (CAS) and peripheral anionic sites (PAS) of AChE. Moreover, compound 5e also inhibited self- or AChE-induced β-amyloid(1-40) aggregation, as well as had potent neuroprotective effects against H(2)O(2)- and glutamate- induced cell death with low toxicity in HT22 cells.Entities:
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Year: 2012 PMID： 22981331 DOI： 10.1016/j.bmcl.2012.08.036
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823