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学科主题: 生命有机化学
题名: 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
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
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)
通讯作者: DEADMAN JOHN JOSEPH ; 谢欣 ; 马大为
刊名: Bioorg. Med. Chem. Lett.
发表日期: 2010
卷: 20, 期:17, 页:5334-5336
收录类别: SCI
部门归属: 中国科学院上海生命科学研究院生化所; Avexa公司; 中国科学院上海药物研究所; 上海靶点公司; 中国科学院上海有机化学研究所
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.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000281247000077
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/15631
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
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.
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