Design, Synthesis, and Biological Evaluation of Novel 6<i>H</i>-Benzo[<i>c</i>]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors
Urolithins (hydroxylated 6<i>H</i>-benzo[<i>c</i>]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 6<i>...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2021-05-01
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| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/22/11/5680 |
| Summary: | Urolithins (hydroxylated 6<i>H</i>-benzo[<i>c</i>]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 6<i>H</i>-benzo[<i>c</i>]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6<i>H</i>-benzo[<i>c</i>]chromen-6-one derivative <b>1f</b> was found to have the optimal inhibitory potential (IC<sub>50</sub>: 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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| ISSN: | 1661-6596 1422-0067 |