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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Detalles Bibliográficos
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
Descripción
Sumario: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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