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 B(李本) ; JONES ERIC DALE ; ZHOU ENKUN ; CHEN LI ; BAYLIS DEAN CAMERON ; Yu SH(余尚海) ; Wang M(汪淼) ; HE XING ; COATES JONATHAN ALAN VICTOR ; RHODES DAVID IAN ; Pei G(裴刚) ; DEADMAN JOHN JOSEPH ; Xie X(谢欣) ; Ma DW(马大为) |
| 刊名 | Bioorg. Med. Chem. Lett.
 |
| 出版日期 | 2010 |
| 卷号 | 20期号:17页码:5334-5336 |
| ISSN号 | 0960-894X |
| 其他题名 | 含1,3,3,4-四取代吡咯烷的CCR5受体拮抗剂的构效关系研究, 第二部分: 高度有效的抗-HIV试剂的发现 |
| 通讯作者 | DEADMAN JOHN JOSEPH ; 谢欣 ; 马大为 |
| 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. |
| 学科主题 | 生命有机化学 |
| 收录类别 | SCI |
| 原文出处 | http://dx.doi.org/10.1016/j.bmcl.2010.05.046 |
| 语种 | 英语 |
| WOS记录号 | WOS:000281247000077 |
| 公开日期 | 2013-02-19 |
| 源URL | [http://202.127.28.38/handle/331003/15631]  |
| 专题 | 上海有机化学研究所_生命有机化学国家重点实验室 |
| 推荐引用方式 GB/T 7714 | Li B,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]. Bioorg. Med. Chem. Lett.,2010,20(17):5334-5336. |
| APA | 李本.,JONES ERIC DALE.,ZHOU ENKUN.,CHEN LI.,BAYLIS DEAN CAMERON.,...&马大为.(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.Bioorg. Med. Chem. Lett.,20(17),5334-5336. |
| MLA | 李本,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".Bioorg. Med. Chem. Lett. 20.17(2010):5334-5336. |
入库方式： OAI收割
来源：上海有机化学研究所
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