Journal
ACS CHEMICAL NEUROSCIENCE
Volume 5, Issue 10, Pages 952-962Publisher
AMER CHEMICAL SOC
DOI: 10.1021/cn500119g
Keywords
Alzheimers disease; selenium-containing clioquinol derivatives; antioxidative properties; inhibition of metal-induced A beta aggregation
Funding
- Natural Science Foundation of China [21302235, 20972198]
- Ph.D. Programs Foundation of the Ministry of Education of China [20120171120045]
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A series of selenium-containing clioquinol derivatives were designed, synthesized, and evaluated as multifunctional anti-Alzheimer's disease (AD) agents. In vitro examination showed that several target compounds exhibited activities such as inhibition of metal-induced A beta aggregation, antioxidative properties, hydrogen peroxide scavenging, and the prevention of copper redox cycling. A parallel artificial membrane permeation assay indicated that selenium-containing clioquinol derivatives possessed significant blood-brain barrier (BBB) permeability. Compound 8a, with a propynylselanyl group linked to the oxine, demonstrated higher hydrogen peroxide scavenging and intracellular antioxidant activity than clioquinol. Furthermore, 8a exhibited significant inhibition of Cu(II)-induced A beta 1-42 aggregation and was capable of disassembling the preformed Cu(II)-induced A beta aggregates. Therefore, 8a is an excellent multifunctional promising compound for development of novel drugs for AD.
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