期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 19, 页码 5884-5892出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.07.045
关键词
Alzheimer's disease; Multifunctional drug candidates; Biometals chelators; Inhibitors of cholinesterases; Antioxidants
资金
- Natural Science Foundation of China [20972198, 81274028]
In an effort to identify novel multifunctional drug candidates for the treatment of Alzheimer's disease (AD), a series of hybrid molecules were synthesised by reacting N-(aminoalkyl)tacrine with salicylic aldehyde or derivatives of 2-aminobenzaldehyde. These compounds were then evaluated as multifunctional anti-Alzheimer's disease agents. All of the hybrids are potential biometal chelators, and in addition, most of them were better antioxidants and inhibitors of cholinesterases and amyloid-beta (A beta) aggregation than the lead compound tacrine. Compound 7c has the potential to be a candidate for AD therapy: it is a much better inhibitor of acetylcholinesterase (AChE) than tacrine (IC50: 0.55 nM vs 109 nM), has good biometal chelation ability, is able to inhibit A beta aggregation and has moderate antioxidant activity (1.22 Trolox equivalents). (C) 2012 Elsevier Ltd. All rights reserved.
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