Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5
文献类型：期刊论文
| 作者 | Gong, Xudong2; Wang, Guan3; Ren, Jing3; Liu, Zheng1; Wang, Zhen3 ; Chen, Tiantian3; Yang, Xiaojun1; Jiang, Xiangrui3; Shen, Jingshan3; Jiang, Hualiang3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2013-09-01 |
| 卷号 | 23期号:17页码:4944-4947 |
| 关键词 | PDE5 inhibitors 5-Bromopyrimidin-4(3H)-ones |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2013.06.062 |
| 文献子类 | Article |
| 英文摘要 | 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. |
| WOS关键词 | DRUG DEVELOPMENT ; PHOSPHODIESTERASE-5 ; DESIGN |
| 资助项目 | '100 Talents Project' of CAS[00000000] ; National Science and Technology Major Project[2011ZX09102-005-02] ; National Science and Technology Major Project[2012ZX09301001-001] ; National High Technology Research and Development Program of China[2012AA020302] ; National Natural Science Foundation of China[91013010] ; National Natural Science Foundation of China[21172233] ; Innovation Fund for Technology Based Firms of Shanghai City[1002H117400] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000323187000038 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277488]  |
| 专题 | 药物发现与设计中心 药物化学研究室 科研与新药推进处 |
| 通讯作者 | Aisa, Haji Akber |
| 作者单位 | 1.Vitargeta Therapeut Inc, Plainsboro, NJ 08536 USA 2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Xinjiang Indigenous Med Plants Resource U, Urumiqi 830011, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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