Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593314 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
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 2.80Â 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.
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Authors
Fei Mao, Jianwen Chen, Qi Zhou, Zonghua Luo, Ling Huang, Xingshu Li,