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学科主题: Pharmacology & Pharmacy ; Chemistry
题名: Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5
作者: 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
通讯作者: Aisa, HA
关键词: PDE5 inhibitors ; 5-Bromopyrimidin-4(3H)-ones
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2013
DOI: 10.1016/j.bmcl.2013.06.062
卷: 23, 期:17, 页:4944-4947
收录类别: SCI
资助者: '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
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.
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内容类型: 期刊论文
URI标识: http://ir.xjipc.cas.cn/handle/365002/2637
Appears in Collections:新疆维吾尔自治区植物资源化学重点实验室 _期刊论文

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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

Recommended Citation:
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.
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文件名: Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.pdf
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