期刊
MEDCHEMCOMM
卷 5, 期 5, 页码 609-616出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3md00376k
关键词
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资金
- Program for Changjiang Scholars and Innovative Research Team in University [IRT1193]
- Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)
Considering the complex pathogenesis factors of Alzheimer's disease (AD), the multitarget-directed ligand strategy is expected to provide superior effects to fight AD, instead of the classic one-drug-one-target strategy. Resveratrol, exhibiting important properties against AD, was suggested to be used as a starting compound for the treatment of AD. Based on these reasons, a series of resveratrol derivatives were designed, synthesized and biologically evaluated. Among them, compound 6r, exhibiting moderate cholinesterase inhibition activity (AChE, IC50 = 6.55 mu M; BuChE, IC50 = 8.04 mu M; SI = 1.23), significant inhibition of A beta(42) aggregation (57.78%, at 20 mu M) and acceptable inhibitory activity against monoamine oxidases (MAO-A, IC50 = 17.58 mu M; MAO-B, IC50 = 12.19 mu M), was a potential anti-Alzheimer agent with balanced activities. Consequently, this study provided useful information for further development of resveratrol derivatives as multitarget-directed agents for AD therapy.
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