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

ABSTRACT: A series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by ¹H NMR, ¹³C 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 IC₅₀ 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.

SUBMITTER: Tang L

PROVIDER: S-EPMC8664850 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature

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

Tang Long L Jiang Jianchun J Song Guoqiang G Wang Yajing Y Zhuang Ziheng Z Tan Ying Y Xia Yan Y Huang Xianfeng X Feng Xiaoqing X

Scientific reports 20211210 1

A series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C 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 ...[more]

PMID: 34893678

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