Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 28, Issue 7, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2020.115374
Keywords
Alzheimer's disease; Flurbiprofen-clioquinol hybrids; Anti-A beta-aggregation; Biometal chelating; Antioxidantion; Anti-neuroinflammation
Funding
- Sichuan Science and Technology Program [2018SZ0014, 2019YFS0088]
- Fundamental Research Funds for the Central Universities
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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 beta-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.
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