Design,Synthesis, and Biological Evaluation of Novel 6H-Benzo[c]chromen-6-one Derivatives as Potential Phosphodiesterase II Inhibitors |
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| Authors: | Long Tang Jianchun Jiang Guoqiang Song Yajing Wang Ziheng Zhuang Ying Tan Yan Xia Xianfeng Huang Xiaoqing Feng |
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| Affiliation: | 1.Institute of Chemical Industry of Forest Products, Chinese Academy of Forestry, Nanjing 210042, China;2.School of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China;3.School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou 213164, China; (G.S.); (Y.W.); (Z.Z.); (Y.T.); (Y.X.); (X.H.) |
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| Abstract: | Urolithins (hydroxylated 6H-benzo[c]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 6H-benzo[c]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6H-benzo[c]chromen-6-one derivative 1f was found to have the optimal inhibitory potential (IC50: 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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| Keywords: | alkoxylated 6H-benzo[c]chromen-6-one phosphodiesterase II inhibitors biological activities |
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