Discovery of novel (S)-alpha-phenyl-gamma-amino butanamide containing CCR5 antagonists via functionality inversion approach
文献类型：期刊论文
| 作者 | Zhang, Hu-Shan1; Feng, Dong-Zhi1; Chen, Li2; Long, Ya-Qiu1 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2010-04-01 |
| 卷号 | 20期号:7页码:2219-2223 |
| 关键词 | CCR5 antagonist HIV-1 entry inhibitor Functionality inversion Bioisostere Butanamide Tropane 2-Methyl-3H-imidazo[4,5-b]pyridine 3H-[1,2,3]Triazolo[4,5-b]pyridine |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2010.02.023 |
| 文献子类 | Article |
| 英文摘要 | By using functionality inversion approach, we identified a new scaffold containing (S)-alpha-phenyl-gamma-amino butanamide as CCR5 antagonists derived from the 1,3-propanediamine carboxamide pharmacophore protocol. The (2S)-2-phenyl-4-(8-aza-bicyclo[3.2.1]octan-8-yl)-butanamide derivatives display significantly high potency to antagonize CCR5 receptor with nanomolar IC50 values. (C) 2010 Elsevier Ltd. All rights reserved. |
| WOS关键词 | MOLECULAR-INTERACTIONS ; POTENT ; INHIBITORS ; INFECTION ; MARAVIROC ; ENTRY ; AGENT |
| 资助项目 | National Natural Science Foundation of China[30672528] ; Science and Technology Commission of Shanghai Municipality[07QH14018] ; Science and Technology Commission of Shanghai Municipality[08JC1422200] ; National Science & Technology Major[2009ZX09301-001] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000275805900036 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278927]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Long, Ya-Qiu |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China; 2.Shanghai TargetDrug Co Ltd, Shanghai 200233, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Hu-Shan,Feng, Dong-Zhi,Chen, Li,et al. Discovery of novel (S)-alpha-phenyl-gamma-amino butanamide containing CCR5 antagonists via functionality inversion approach[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(7):2219-2223. |
| APA | Zhang, Hu-Shan,Feng, Dong-Zhi,Chen, Li,&Long, Ya-Qiu.(2010).Discovery of novel (S)-alpha-phenyl-gamma-amino butanamide containing CCR5 antagonists via functionality inversion approach.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(7),2219-2223. |
| MLA | Zhang, Hu-Shan,et al."Discovery of novel (S)-alpha-phenyl-gamma-amino butanamide containing CCR5 antagonists via functionality inversion approach".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.7(2010):2219-2223. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
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。