Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

A series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by (1)H NMR, (13)C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydr...

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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: Nature Publishing Group UK 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8664850/
https://www.ncbi.nlm.nih.gov/pubmed/34893678
http://dx.doi.org/10.1038/s41598-021-03194-y
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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 A series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by (1)H NMR, (13)C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC(50) of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.
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spelling pubmed-86648502021-12-13 Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors Tang, Long Jiang, Jianchun Song, Guoqiang Wang, Yajing Zhuang, Ziheng Tan, Ying Xia, Yan Huang, Xianfeng Feng, Xiaoqing Sci Rep Article A series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by (1)H NMR, (13)C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC(50) of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity. Nature Publishing Group UK 2021-12-10 /pmc/articles/PMC8664850/ /pubmed/34893678 http://dx.doi.org/10.1038/s41598-021-03194-y Text en © The Author(s) 2021 https://creativecommons.org/licenses/by/4.0/Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (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 urolithins derivatives as potential phosphodiesterase II inhibitors
title Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors
title_full Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors
title_fullStr Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors
title_full_unstemmed Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors
title_short Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors
title_sort design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase ii inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8664850/
https://www.ncbi.nlm.nih.gov/pubmed/34893678
http://dx.doi.org/10.1038/s41598-021-03194-y
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