Novel tacrine–ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity

F Mao, J Chen, Q Zhou, Z Luo, L Huang, X Li

文献索引：Mao, Fei; Chen, Jianwen; Zhou, Qi; Luo, Zonghua; Huang, Ling; Li, Xingshu Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6737 - 6742

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被引用次数: 18

摘要

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 IC 50 values of 2.55 and 2.80 nM, respectively. Furthermore, this compound demonstrated ...