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

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 s...

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Detalles Bibliográficos
Autores principales: Chen, Liang-Chieh, Hsu, Kai-Cheng, Chiou, Lih-Chu, Tseng, Hui-Ju, Huang, Wei-Jan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150239/
https://www.ncbi.nlm.nih.gov/pubmed/29113055
http://dx.doi.org/10.3390/molecules22111897
Descripción
Sumario: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.