XJIPC OpenIR  > 省部共建新疆特有药用资源利用重点实验室
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5
Gong Xudong; Wang Guan; Ren Jing; Liu Zheng; Wang Zhen; Chen Tiantian; Yang Xiaojun; Jiang Xiangrui; Shen Jingshan; Jiang Hualiang; Aisa Haji Akber; Xu Yechun; Li Jianfeng; Aisa, HA
2013
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume23Issue:17Pages:4944-4947
Abstract

The substituents both at the 6-position of the 5-bromopyrimidinone ring and at the 5'-position of the phenyl ring of 5-bromopyrimidin-4(3H)-ones were explored. 5-Bromo-6-isopropyl-2-(2-propoxyphenyl)pyrimidin-4(3H)-one was identified as a new scaffold for potent PDE5 inhibitors. The crystal structures of PDE5/2e and PDE5/10a complexes provided a structural basis for the inhibition of 5-bromopyrimidinones to PDE5. In addition, it was also found that there is a great tolerance for the substitution at the 5'-position of the phenyl ring of 5-bormopyrimidinones and the resulted compound 13a has the highest inhibition activity to PDE5 (IC50, 1.7 nM).

KeywordPde5 Inhibitors 5-bromopyrimidin-4(3h)-ones
Subject AreaPharmacology & Pharmacy ; Chemistry
DOI10.1016/j.bmcl.2013.06.062
Indexed BySCI
WOS IDWOS:000323187000038
Citation statistics
Cited Times:6[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/2637
Collection省部共建新疆特有药用资源利用重点实验室
Corresponding AuthorAisa, HA
AffiliationChinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Xinjiang Indigenous Med Plants Resource U, Urumiqi 830011, Peoples R China;Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China;Vitargeta Therapeut Inc, Plainsboro, NJ 08536 USA
Recommended Citation
GB/T 7714
Gong Xudong,Wang Guan,Ren Jing,et al. Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2013,23(17):4944-4947.
APA Gong Xudong.,Wang Guan.,Ren Jing.,Liu Zheng.,Wang Zhen.,...&Aisa, HA.(2013).Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,23(17),4944-4947.
MLA Gong Xudong,et al."Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 23.17(2013):4944-4947.
Files in This Item:
File Name/Size DocType Version Access License
Exploration of the 5(2158KB)期刊论文作者接受稿开放获取CC BY-NC-SAView Application Full Text
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Gong Xudong]'s Articles
[Wang Guan]'s Articles
[Ren Jing]'s Articles
Baidu academic
Similar articles in Baidu academic
[Gong Xudong]'s Articles
[Wang Guan]'s Articles
[Ren Jing]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Gong Xudong]'s Articles
[Wang Guan]'s Articles
[Ren Jing]'s Articles
Terms of Use
No data!
Social Bookmark/Share
File name: Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.pdf
Format: Adobe PDF
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.