Purin-6-One Derivatives as Phosphodiesterase-2 Inhibitors
Joint Authors
Yuan, Wei
Zhao, Xin-Yun
Chen, Xi
Zhan, Chang-Guo
Source
Issue
Vol. 2016, Issue 2016 (31 Dec. 2016), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2016-02-22
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
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 IC50 values of 1.73, 0.18, and 3.43 μM, 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.
American Psychological Association (APA)
Yuan, Wei& Zhao, Xin-Yun& Chen, Xi& Zhan, Chang-Guo. 2016. Purin-6-One Derivatives as Phosphodiesterase-2 Inhibitors. Journal of Chemistry،Vol. 2016, no. 2016, pp.1-10.
https://search.emarefa.net/detail/BIM-1107740
Modern Language Association (MLA)
Yuan, Wei…[et al.]. Purin-6-One Derivatives as Phosphodiesterase-2 Inhibitors. Journal of Chemistry No. 2016 (2016), pp.1-10.
https://search.emarefa.net/detail/BIM-1107740
American Medical Association (AMA)
Yuan, Wei& Zhao, Xin-Yun& Chen, Xi& Zhan, Chang-Guo. Purin-6-One Derivatives as Phosphodiesterase-2 Inhibitors. Journal of Chemistry. 2016. Vol. 2016, no. 2016, pp.1-10.
https://search.emarefa.net/detail/BIM-1107740
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1107740