Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer’s disease |
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| Institution: | 1. Middle Tennessee State University, Department of Biology, 1301 East Main Street, Murfreesboro, TN 37132, USA;2. Middle Tennessee State University, Department of Chemistry, 1301 East Main Street, Murfreesboro, TN 37132, USA |
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| Abstract: | A series of 4-hydroxyl aurone derivatives were designed synthesized and evaluated as potential multifunctional agents for the treatment of Alzheimer’s disease. The results demonstrated that most of the derivatives exhibited good multifunctional properties. Among them, compound 14e displayed good inhibitory activities of self- and Cu2+-induced Aβ1–42 aggregation with 99.2% and 84.0% at 25 μM, respectively, and high antioxidant activity with a value 1.90-fold of Trolox. In addition, 14e also showed remarkable inhibitory activities of both monoamine oxidase A and B with IC50 values of 0.271 μM and 0.393 μM, respectively. However the 6-methoxyl aurones 15a–c revealed excellent selectivity toward MAO-B. Furthermore, the representative compounds 14e and 15b displayed good metal-chelating abilities and blood–brain barrier (BBB) permeabilities in vitro. |
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| Keywords: | Alzheimer’s disease Aurone derivatives Multifunctional agents Monoamine oxidase |
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