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Design, Synthesis and Pharmacological Evaluation of Novel Tacrine-Caffeic Acid Hybrids as Multi-Targeted Compounds Against Alzheimer's Disease

Design, Synthesis and Pharmacological Evaluation of Novel Tacrine-Caffeic Acid Hybrids as Multi-Targeted Compounds Against Alzheimer's Disease

Xiaojuan Chao, 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

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6498-502.

PMID: 22981331

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP331395-A	Caffeic Acid - CAS 331-39-5		331-39-5	Price

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