中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
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
DOI10.1016/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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