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J Enzyme Inhib Med Chem. 2019 Dec;34(1):1489-1497. doi: 10.1080/14756366.2019.1634703.

Dual-target anti-Alzheimer's disease agents with both iron ion chelating and monoamine oxidase-B inhibitory activity.

Author information

1
a College of Pharmaceutical Science, Zhejiang University of Technology , Hangzhou , China.
2
b Guiyang Institute for Food and Drug Control , Guiyang , China.
3
c Department of Pathophysiology, College of Basic Medical Sciences, Jilin University , Changchun , China.
4
d School of Food Science and Biotechnology, Zhejiang Gongshang University , Hangzhou , China.
5
e Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology , Hangzhou , China.

Abstract

MAO-B leads to an increase in the levels of hydrogen peroxide and oxidative free radicals, which contribute to the aetiology of the AD. Thus, both iron ion chelators and MAO-B inhibitors can be used to treat AD. Taking the coumarin derivatives and hydroxypyridinones as the lead compounds, a series of dual-target hybrids were designed and synthesised by Click Chemistry. The compounds were biologically evaluated for their iron ion chelating and MAO-B inhibitory activity. Most of the compounds displayed excellent iron ion chelating activity and moderate to good anti-MAO-B activity. Compounds 27b and 27j exhibited the most potent MAO-B inhibitory activity, with IC50 values of 0.68 and 0.86 μM, respectively. In summary, these dual-target compounds have the potential anti-AD activity.

KEYWORDS:

Alzheimer’s disease; MAO-B; coumarin derivatives; hydroxypyridinone; iron ion chelation

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