Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents
文献类型：期刊论文
| 作者 | Ben, Li2; Jones, Eric Dale3; Zhou, Enkun1; Li, Chen4; Baylis, Dean Cameron3; Yu, Shanghai5; Wang, Miao5; He, Xing1; Coates, Jonathan Alan Victor3; Rhodes, David Ian3 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2010-07-15 |
| 卷号 | 20期号:14页码:4012-4014 |
| 关键词 | CCR5 antagonists Anti-HIV |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2010.05.102 |
| 文献子类 | Article |
| 英文摘要 | A novel series of CCR5 antagonists has been identified, utilizing the lead, nifeviroc, which were further modified based on bioisosteric principles. Lead optimization was pursued by balancing potential toxicity and potency. Potent analogues with low toxic properties were successfully developed by formation of urea and amide bonds at the nitrogen at position 4- of the pyrrolidine ring. (C) 2010 Elsevier Ltd. All rights reserved. |
| WOS关键词 | SMALL-MOLECULE ; HIV-1 INHIBITORS ; POTENT ; DISCOVERY ; INFECTION ; 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:000279258800002 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278832]  |
| 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 | Xie, Xin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai 200031, Peoples R China; 3.Avexa Ltd, Richmond, Vic 3121, Australia; 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 | Ben, Li,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 1: Tuning the N-substituents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(14):4012-4014. |
| APA | Ben, Li.,Jones, Eric Dale.,Zhou, Enkun.,Li, Chen.,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 1: Tuning the N-substituents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(14),4012-4014. |
| MLA | Ben, Li,et al."Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.14(2010):4012-4014. |
入库方式： OAI收割
来源：上海药物研究所
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