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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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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
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author Chen, Liang-Chieh
Hsu, Kai-Cheng
Chiou, Lih-Chu
Tseng, Hui-Ju
Huang, Wei-Jan
author_facet Chen, Liang-Chieh
Hsu, Kai-Cheng
Chiou, Lih-Chu
Tseng, Hui-Ju
Huang, Wei-Jan
author_sort Chen, Liang-Chieh
collection PubMed
description 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.
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spelling pubmed-61502392018-11-13 Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative Chen, Liang-Chieh Hsu, Kai-Cheng Chiou, Lih-Chu Tseng, Hui-Ju Huang, Wei-Jan Molecules Article 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. MDPI 2017-11-04 /pmc/articles/PMC6150239/ /pubmed/29113055 http://dx.doi.org/10.3390/molecules22111897 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Chen, Liang-Chieh
Hsu, Kai-Cheng
Chiou, Lih-Chu
Tseng, Hui-Ju
Huang, Wei-Jan
Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative
title Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative
title_full Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative
title_fullStr Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative
title_full_unstemmed Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative
title_short Total Synthesis and Metabolic Stability of Hispidulin and Its d-Labelled Derivative
title_sort total synthesis and metabolic stability of hispidulin and its d-labelled derivative
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150239/
https://www.ncbi.nlm.nih.gov/pubmed/29113055
http://dx.doi.org/10.3390/molecules22111897
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