期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 4, 页码 1355-1361出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.12.066
关键词
GPx mimics; Cholinesterase inhibitors; Alzheimer's disease
资金
- Natural Science Foundation of China [21302235, 20972198]
- Ph.D. Programs Foundation of the Ministry of Education of China [20120171120045]
- Distinguished Young Talents in Higher Education of Guangdong [2012LYM_003]
A series of ebselen derivatives were designed, synthesised and evaluated as inhibitors of cholinesterases (ChEs) and glutathione peroxidase (GPx) mimics. Most of the compounds were found to be potent against AChEs and BuChE, compounds 5e and 5i, proved to be the most potent against AChE with IC50 values of 0.76 and 0.46 mu M, respectively. Among these hybrids, most of the compounds were found to be good GPx mimics compare with ebselen. The selected compounds 5e and 5i were also used to determine the catalytic parameters and in vitro hydrogen peroxide scavenging activity. The results indicate that compounds 5e and 5i may be excellent multifunctional agents for the treatment of AD. (C) 2014 Elsevier Ltd. All rights reserved.
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