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- W2287659744 abstract "A series of purin-6-one derivatives were synthesized, and their in vitro inhibitory activity against phosphodiesterase-2 (PDE2) was evaluated by using a fluorescence polarization assay. Three compounds, that are, 2j , 2p , and 2q , showed significant inhibitory activity against PDE2 with IC 50 values of 1.73, 0.18, and 3.43 μ M, respectively. Structure-activity relationship (SAR) analysis was performed to explore the relationship between the chemical structures of these compounds and their inhibitory activity. Compounds 2j , 2p , and 2q were further selected for molecular docking study. The docking results suggested that these ligands bind with hydrophobic pockets of the catalytic active site of PDE2, where a Tyr655 residue was found to be important in binding with compound 2p , the most potent inhibitor identified in this study. Our present study provides useful information for the future design of novel PDE2 inhibitors." @default.
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- W2287659744 date "2016-01-01" @default.
- W2287659744 modified "2023-10-15" @default.
- W2287659744 title "Purin-6-One Derivatives as Phosphodiesterase-2 Inhibitors" @default.
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- W2287659744 doi "https://doi.org/10.1155/2016/6878353" @default.
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