Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5

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	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
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2013
卷号	23 期号:17 页码:4944-4947
关键词	PDE5 inhibitors 5-Bromopyrimidin-4(3H)-ones
ISSN号	0960-894X
通讯作者	Aisa, HA
中文摘要	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). (C) 2013 Elsevier Ltd. All rights reserved.
学科主题	Pharmacology & Pharmacy ; Chemistry
收录类别	SCI
资助信息	'100 Talents Project' of CAS; National Science and Technology Major Project 2011ZX09102-005-02, 2012ZX09301001-001; National High Technology Research and Development Program of China 2012AA020302; National Natural Science Foundation of China 91013010, 21172233; Innovation Fund for Technology Based Firms of Shanghai City 1002H117400
公开日期	2013-11-07
内容类型	期刊论文
源URL	[http://ir.xjipc.cas.cn/handle/365002/2637]
专题	新疆理化技术研究所_省部共建新疆特有药用资源利用重点实验室
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.,...&Li Jianfeng.(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.