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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2017
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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. |
format | Online Article Text |
id | pubmed-6150239 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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