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Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.

Abstract：

:A series of novel flurbiprofen-clioquinol hybrids were designed and synthesized as multifunctional agents for Alzheimer's disease therapy, and their potential was evaluated through various biological experiments. In vitro studies showed that most target compounds exhibited significant ability to inhibit self- and Cu2+-induced β-amyloid aggregation. Furthermore, some target compounds, especially 7i and 7r, also showed biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activity and appropriate BBB permeability. These biological activities indicated that the representative compound 7i and 7r might be promising multifunctional agents for AD treatment.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Yang Z,Song Q,Cao Z,Yu G,Liu Z,Tan Z,Deng Y

doi

10.1016/j.bmc.2020.115374

subject

Has Abstract

pub_date

2020-04-01 00:00:00

pages

115374

issue

7

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(20)30170-X

journal_volume

28

pub_type

杂志文章

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