期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 23, 期 1, 页码 231-240出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.11.004
关键词
Acetylcholinesterase inhibitor; Alzheimer's disease; Aurone; Galantamine; Memory enhancing; Sulfuretin
资金
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - MEST, Republic of Korea [2012-006431]
Alzheimer's disease (AD), a progressive and neurodegenerative disorder of the brain, is the most common cause of dementia among elderly people. To date, the successful therapeutic strategy to treat AD is maintaining the levels of acetylcholine by inhibiting acetylcholinesterase (AChE). In the present study, aurone derivatives were designed and synthesized as AChE inhibitors based on the lead structure of sulfuretin. Of those synthesized, compound 10d showed ca. 1700-fold and 6-fold higher AChE inhibitory activity than sulfuretin and galantamine, respectively. This compound also ameliorated scopolamine-induced memory deficit in mice when administered orally at the dose of 1 and 2 mg/kg. (C) 2014 Published by Elsevier Ltd.
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