期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 81, 期 -, 页码 15-21出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.05.002
关键词
Alzheimer's disease; Butyrylcholinesterase inhibitor; Neuroprotection; Evodiamine; Carbamates
资金
- German Science Foundation (Deutsche Forschungsgemeinschaft) [DFG DE1546/6-1]
Two sets of carbamates based on the natural alkaloid evodiamine were designed, synthesized and evaluated as potential butyrylcholinesterase inhibitors. Although a set of carbamates of 3-hydroxyevodiamine (10a-f) is inactive both at AChE and BChE, carbamates of 5-deoxo-3-hydroxyevodiamine (11a-f) exhibit much better potency with selectivity toward BChE. The heptyl carbamate of 5-deoxo-3-hydroxyevodiamine (11c) shows the best potency with an IC50 value of 77 nM and very good selectivity over AChE. ORAC and cell-based assays indicate 11c owns pronounced antioxidant properties with 1.75 Trolox equivalents and strong neuroprotection even from 1 mu M onwards. These combined activities might enable compound 11c to be a potential candidate for treatment of Alzheimer's disease. (C) 2014 Elsevier Masson SAS. All rights reserved.
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