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Discovery of boron-containing compounds as Aβ aggregation inhibitors and antioxidants for the treatment of Alzheimer's disease

Abstract

A novel series of boron-containing compounds were designed, synthesized and evaluated as multi-target-directed ligands against Alzheimer's disease. Biological activity results demonstrated that these compounds possessed a significant ability to inhibit self-induced Aβ aggregation (20.5-82.8%, 20 µM) and to act as potential antioxidants (oxygen radical absorbance capacity assay using fluorescein (ORAC-FL) values of 2.70-5.87). In particular, compound 17h is a potential lead compound for AD therapy (IC50 = 3.41 μM for self-induced Aβ aggregation; ORAC-FL value = 4.55). Compound 17h also functions as a metal chelator. These results indicated that boron-containing compounds could be new structural scaffolds for the treatment of AD.

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Publication details

The article was received on 26 Jun 2018, accepted on 09 Sep 2018 and first published on 12 Sep 2018


Article type: Research Article
DOI: 10.1039/C8MD00315G
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Discovery of boron-containing compounds as Aβ aggregation inhibitors and antioxidants for the treatment of Alzheimer's disease

    C. Lu, J. Hu, Z. Wang, S. Xie, T. Pan, L. Huang and X. Li, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00315G

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