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Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimer's Disease Candidates Based on Metabolic Mechanism

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In order to improve the metabolic stability and bioavailability of scutellarin, some derivatives of its main metabolite (scutellarein) were designed and synthesized. The antioxidant activities of these target products were assessed by measuring its scavenging capacities toward DPPH and the protective effects on H2O2-induced cytotoxicity in PC12 cells. The results showed that the target compound 7g had a higher antioxidant activity than scutellarin. Thus 7g may be considered as a novel potent anti-Alzheimer's Disease drug candidate.

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Keywords: Alzheimer's disease; Alzheimer's disease (AD); Antioxidant; DPPH; Derivative; Metabolism; PC12; Scutellarein; Scutellarin; Synthesize; amyloid β protein; anti-Alzheimer's Disease drug candidate; cytotoxicity; neuroprotection; pathophysiological; peroxynitrate; scutellarein

Document Type: Research Article

Publication date: January 1, 2012

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.
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