期刊
CHEMISTRYSELECT
卷 3, 期 2, 页码 461-466出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201702781
关键词
Alzheimer's disease; Biological Evaluation; Molecular Modeling; Synthesis; QuinoPyranoTacrines
资金
- Regional Council of Franche-Comte [2016YC-04540, 2016YC-04560]
- Faculty of Military Health Sciences, University of Defence, MH CZ - DRO (UHHK) [00179906]
- MINECO (Spain) [SAF2015-65586-R]
- EU (COST Action CA15135: Multi-target paradigm for innovative ligand identification in the drug discovery process)
- Long Term Development Plan - 1011
In this report we describe the synthesis, biological evaluation and molecular modeling of new tacrine analogues such as QuinoPyranTacrines (QPTs), designed by juxtaposition of 1,4-naphthoquinone and tacrine. From these results we have identified QPT16 as a permeable, selective human acetylcholinesterase inhibitor [IC50= 1.1 +/- 0.15 mu M], 3.5-fold less-hepatotoxic than tacrine at 1000 mu M concentration, and consequently, a potential new hit-compound for further investigation targeted to find a new agent for AD therapy.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据