期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 23, 页码 7406-7417出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.09.050
关键词
Alzheimer's disease; Cholinesterase; Monoamine oxidase-B
资金
- National Natural Science Foundation of China [21302235]
- Distinguished Young Talents in Higher Education of Guangdong [2012LYM_003]
- Ph.D. Programs Foundation of Ministry of Education of China [20120171120045]
- Guangdong Engineering Research Center of Chiral Drugs
A series of Tacrine-Homoisoflavonoid hybrids were designed, synthesised and evaluated as inhibitors of cholinesterases (ChEs) and human monoamine oxidases (MAOs). Most of the compounds were found to be potent against both ChEs and MAO-B. Among these hybrids, compound 8b, with a 6 carbon linker between tacrine and (E)-7-hydroxy-3-(4-methoxybenzylidene)chroman-4-one, proved to be the most potent against AChE and MAO-B with IC50 values of 67.9 nM and 0.401 mu M, respectively. This compound was observed to cross the blood-brain barrier (BBB) in a parallel artificial membrane permeation assay for the BBB (PAMPA-BBB). The results indicated that compound 8b is an excellent multifunctional promising compound for development of novel drugs for Alzheimer's disease (AD). (C) 2013 Elsevier Ltd. All rights reserved.
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