Dual-target anti-Alzheimer's disease agents with both iron ion chelating and monoamine oxidase-B inhibitory activity
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 o...
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Taylor & Francis Group,
2019-01-01T00:00:00Z.
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| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_b1ce88235d8d42e094f79c1103d7a902 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Zhisheng Mi |e author |
| 700 | 1 | 0 | |a Bing Gan |e author |
| 700 | 1 | 0 | |a Sihang Yu |e author |
| 700 | 1 | 0 | |a Jianan Guo |e author |
| 700 | 1 | 0 | |a Changjun Zhang |e author |
| 700 | 1 | 0 | |a Xiaoying Jiang |e author |
| 700 | 1 | 0 | |a Tao Zhou |e author |
| 700 | 1 | 0 | |a Jing Su |e author |
| 700 | 1 | 0 | |a Renren Bai |e author |
| 700 | 1 | 0 | |a Yuanyuan Xie |e author |
| 245 | 0 | 0 | |a Dual-target anti-Alzheimer's disease agents with both iron ion chelating and monoamine oxidase-B inhibitory activity |
| 260 | |b Taylor & Francis Group, |c 2019-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2019.1634703 | ||
| 520 | |a 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. | ||
| 546 | |a EN | ||
| 690 | |a alzheimer's disease | ||
| 690 | |a iron ion chelation | ||
| 690 | |a mao-b | ||
| 690 | |a coumarin derivatives | ||
| 690 | |a hydroxypyridinone | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 1489-1497 (2019) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2019.1634703 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/b1ce88235d8d42e094f79c1103d7a902 |z Connect to this object online. |