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

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	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
	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.
	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
内容类型	期刊论文
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.