A small bifunctional chelator that modulates Aβ42 aggregation

Autor:	Tonglu Zhang, Chaofeng Zhang, Luiza M.F. Gomes, Tim Storr
Rok vydání:	2018
Předmět:	010405 organic chemistry β amyloid Chemistry Metal ions in aqueous solution Organic Chemistry Click chemistry Bifunctional chelator General Chemistry 010402 general chemistry 01 natural sciences Combinatorial chemistry Catalysis 0104 chemical sciences
Zdroj:	Canadian Journal of Chemistry. 96:78-82
ISSN:	1480-3291 0008-4042
DOI:	10.1139/cjc-2017-0623
Popis:	Multifunctional compounds that can modulate amyloid-β (Aβ) aggregation and interact with metal ions hold considerable promise as therapeutic agents for Alzheimer’s disease (AD). Using the copper-catalyzed azide-alkyne cycloaddition reaction, a novel bifunctional chelator 2-(1-(4-(dimethylamino)benzyl)-1H-1,2,3-triazol-4-yl)phenol (L1) was synthesized. L1 contains a bidentate metal-binding unit and a pendant dimethylamino moiety. The product was characterized by 1H NMR, 13C NMR, and MS. The metal-binding properties of L1 were probed by UV–vis spectroscopy to determine Cu:L stoichiometry. L1 was determined to limit Aβ aggregation at 48 h via a ThT assay. In addition, L1 complies with Lipinski’s rules and calculated logBB values for potential drug likeness and BBB permeability. These results suggest that L1 is a suitable candidate for further study as a multifunctional compound to treat AD.
Databáze:	OpenAIRE
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