Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors

Urolithins (hydroxylated 6H-benzo[c]chromen-6-ones) are the main bioavailable metabolites of ellagic acid (EA), which was shown to be a cognitive enhancer in the treatment of neurodegenerative diseases. As part of this research, a series of alkoxylated 6H-benzo[c]chromen-6-one derivatives were desig...

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Autores principales: Tang, Long, Jiang, Jianchun, Song, Guoqiang, Wang, Yajing, Zhuang, Ziheng, Tan, Ying, Xia, Yan, Huang, Xianfeng, Feng, Xiaoqing
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8199001/
https://www.ncbi.nlm.nih.gov/pubmed/34073595
http://dx.doi.org/10.3390/ijms22115680
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author Tang, Long
Jiang, Jianchun
Song, Guoqiang
Wang, Yajing
Zhuang, Ziheng
Tan, Ying
Xia, Yan
Huang, Xianfeng
Feng, Xiaoqing
author_facet Tang, Long
Jiang, Jianchun
Song, Guoqiang
Wang, Yajing
Zhuang, Ziheng
Tan, Ying
Xia, Yan
Huang, Xianfeng
Feng, Xiaoqing
author_sort Tang, Long
collection PubMed
description Urolithins (hydroxylated 6H-benzo[c]chromen-6-ones) are the main bioavailable metabolites of ellagic acid (EA), which was shown to be a cognitive enhancer in the treatment of neurodegenerative diseases. As part of this research, a series of alkoxylated 6H-benzo[c]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6H-benzo[c]chromen-6-one derivative 1f was found to have the optimal inhibitory potential (IC(50): 3.67 ± 0.47 μM). It also exhibited comparable activity in comparison to that of BAY 60-7550 in vitro cell level studies.
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spelling pubmed-81990012021-06-14 Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors Tang, Long Jiang, Jianchun Song, Guoqiang Wang, Yajing Zhuang, Ziheng Tan, Ying Xia, Yan Huang, Xianfeng Feng, Xiaoqing Int J Mol Sci Article Urolithins (hydroxylated 6H-benzo[c]chromen-6-ones) are the main bioavailable metabolites of ellagic acid (EA), which was shown to be a cognitive enhancer in the treatment of neurodegenerative diseases. As part of this research, a series of alkoxylated 6H-benzo[c]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6H-benzo[c]chromen-6-one derivative 1f was found to have the optimal inhibitory potential (IC(50): 3.67 ± 0.47 μM). It also exhibited comparable activity in comparison to that of BAY 60-7550 in vitro cell level studies. MDPI 2021-05-26 /pmc/articles/PMC8199001/ /pubmed/34073595 http://dx.doi.org/10.3390/ijms22115680 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tang, Long
Jiang, Jianchun
Song, Guoqiang
Wang, Yajing
Zhuang, Ziheng
Tan, Ying
Xia, Yan
Huang, Xianfeng
Feng, Xiaoqing
Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors
title Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors
title_full Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors
title_fullStr Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors
title_full_unstemmed Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors
title_short Design, Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors
title_sort design, synthesis, and biological evaluation of novel 6h-benzo[c]chromen-6-one derivatives as potential phosphodiesterase ii inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8199001/
https://www.ncbi.nlm.nih.gov/pubmed/34073595
http://dx.doi.org/10.3390/ijms22115680
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