Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors.
Sci Rep
; 11(1): 23792, 2021 12 10.
Article
em En
| MEDLINE
| ID: mdl-34893678
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Fosfodiesterase
/
Desenho de Fármacos
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Exonucleases
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Técnicas de Química Sintética
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article