Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents
文献类型：期刊论文
| 作者 | Li, Ben2; Jones, Eric Dale1; Zhou, Enkun3; Chen, Li4; Baylis, Dean Cameron1; Yu, Shanghai5; Wang, Miao5; He, Xing3; Coates, Jonathan Alan Victor1; Rhodes, David Ian1 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2010-09-01 |
| 卷号 | 20期号:17页码:5334-5336 |
| 关键词 | CCR5 receptor antagonist Anti-HIV |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2010.05.046 |
| 文献子类 | Article |
| 英文摘要 | Modification of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists revealed that introducing a fluoro group at the 3-position of the 3-phenyl group to reduce metabolism did not adversely affect the high potency against HIV infection, and that replacing the piperidine ring with a tropane ring could deliver the most potent anti-HIV agents. Stereochemistry of the substituted tropane ring is essential for maintaining the potent anti-HIV activity because only exo-isomers displayed subnanomolar whole cell activity. (C) 2010 Elsevier Ltd. All rights reserved. |
| WOS关键词 | IMMUNODEFICIENCY-VIRUS TYPE-1 ; ENTRY |
| 资助项目 | National Natural Science Foundation of China[90713047] ; Ministry of Science and Technology[2008DFB30150] ; Ministry of Science and Technology[2009ZX09302-001] ; Ministry of Science and Technology[2009ZX09501-009] ; Chinese Academy of Sciences[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000281247000077 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278783]  |
| 专题 | 国家新药筛选中心 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 | Deadman, John Joseph |
| 作者单位 | 1.Avexa Ltd, Richmond, Vic 3121, Australia; 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai 200031, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 4.Shanghai Targetdrug Co Ltd, Shanghai 20023, Peoples R China; 5.Chinese Acad Sci, Shanghai Inst Organ Chem, State Key Lab Bioorgan & Nat Prod Chem, Shanghai 200032, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Ben,Jones, Eric Dale,Zhou, Enkun,et al. Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(17):5334-5336. |
| APA | Li, Ben.,Jones, Eric Dale.,Zhou, Enkun.,Chen, Li.,Baylis, Dean Cameron.,...&Ma, Dawei.(2010).Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(17),5334-5336. |
| MLA | Li, Ben,et al."Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.17(2010):5334-5336. |
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。