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
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号23期号:17页码:4944-4947
摘要

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).

关键词Pde5 Inhibitors 5-bromopyrimidin-4(3h)-ones
学科领域Pharmacology & Pharmacy ; Chemistry
DOI10.1016/j.bmcl.2013.06.062
收录类别SCI
WOS记录号WOS:000323187000038
引用统计
被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.xjipc.cas.cn/handle/365002/2637
专题省部共建新疆特有药用资源利用重点实验室
通讯作者Aisa, HA
作者单位Chinese 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
推荐引用方式
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.
条目包含的文件
文件名称/大小 文献类型 版本类型 开放类型 使用许可
Exploration of the 5(2158KB)期刊论文作者接受稿开放获取CC BY-NC-SA浏览 请求全文
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Gong Xudong]的文章
[Wang Guan]的文章
[Ren Jing]的文章
百度学术
百度学术中相似的文章
[Gong Xudong]的文章
[Wang Guan]的文章
[Ren Jing]的文章
必应学术
必应学术中相似的文章
[Gong Xudong]的文章
[Wang Guan]的文章
[Ren Jing]的文章
相关权益政策
暂无数据
收藏/分享
文件名: Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.pdf
格式: Adobe PDF
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。