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Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative.

ABSTRACT: Hispidulin is a naturally occurring flavone known to have various Central nervous system (CNS) activities. Proposed synthetic approaches to synthesizing hispidulin have proven unsatisfactory due to their low feasibility and poor overall yields. To solve these problems, this study developed a novel scheme for synthesizing hispidulin, which had an improved overall yield as well as more concise reaction steps compared to previous methods reported. Additionally, using the same synthetic strategy, d-labelled hispidulin was synthesized to investigate its metabolic stability against human liver microsome. This work may produce new chemical entities for enriching the library of hispidulin-derived compounds.

SUBMITTER: Chen LC

PROVIDER: S-EPMC6150239 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature

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Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative.

Chen Liang-Chieh LC Hsu Kai-Cheng KC Chiou Lih-Chu LC Tseng Hui-Ju HJ Huang Wei-Jan WJ

Molecules (Basel, Switzerland) 20171104 11

Hispidulin is a naturally occurring flavone known to have various Central nervous system (CNS) activities. Proposed synthetic approaches to synthesizing hispidulin have proven unsatisfactory due to their low feasibility and poor overall yields. To solve these problems, this study developed a novel scheme for synthesizing hispidulin, which had an improved overall yield as well as more concise reaction steps compared to previous methods reported. Additionally, using the same synthetic strategy, <i ...[more]

PMID: 29113055

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Dataset Information

Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative.

Publications

Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative.

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