期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 4, 页码 830-833出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.12.071
关键词
Iminosugars; Cholinesterases; Inhibitors; Alzheimer disease
资金
- 'Institut Universitaire de France' (IUF)
- CNRS
- University of Strasbourg
- French Department of Research
- Region Centre
To further extend the scope of iminosugar biological activity, a systematic structure-activity relationship investigation has been performed by synthesizing and evaluating as cholinesterase inhibitors a library of twenty-three iminoalditols with different substitutions and stereochemistry patterns. These compounds have been evaluated in vitro for the inhibition of cholinesterases (different sources of acetylcholinesterase and butyrylcholinesterase). Some compounds have IC50 values in the micromolar range and display significant inhibition selectivity for butyrylcholinesterase over acetylcholinesterase. These are the first examples of iminosugar-based inhibitors of cholinesterases. (C) 2015 Elsevier Ltd. All rights reserved.
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