期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 24, 页码 6737-6742出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.10.034
关键词
Alzheimer's disease; Cholinesterase inhibitor; Antioxidant; Peroxynitrite scavenging activity
资金
- Natural Science Foundation of China [20972198]
- Guangdong Engineering Research Center of Chiral Drugs
A series of tacrine-ebselen hybrids were synthesised and evaluated as possible multifunctional anti-Alzheimer's disease (AD) agents. Compound 6i, which is tacrine linked with 5,6-dimethoxybenzo[d][1,2]selenazol-3(2H)-one by a six-carbon spacer, was the most potent acetylcholinesterase (AChE) and butylcholinesterase (BuChE) inhibitor, with IC50 values of 2.55 and 2.80 nM, respectively. Furthermore, this compound demonstrated similar hydrogen peroxide and peroxynitrite scavenging activity as ebselen by horseradish peroxidase assay and peroxynitrite scavenging activity assay, indicating that this hybrid is a good multifunctional drug candidate for the treatment of AD. (C) 2013 Elsevier Ltd. All rights reserved.
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