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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2010-8-16
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AHH,
pubmed-author:BaylisDean CameronDC,
pubmed-author:ChanC RCR,
pubmed-author:ChenLiL,
pubmed-author:CoatesJonathan Alan VictorJA,
pubmed-author:DeadmanJohn JosephJJ,
pubmed-author:HeXingX,
pubmed-author:JonesEric DaleED,
pubmed-author:LiBenB,
pubmed-author:MaDaweiD,
pubmed-author:RhodesDavid IanDI,
pubmed-author:WangMiaoM,
pubmed-author:YuShanghaiS,
pubmed-author:ZhouEnkunE
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5334-6
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pubmed:meshHeading |
pubmed-meshheading:20674358-Animals,
pubmed-meshheading:20674358-Anti-HIV Agents,
pubmed-meshheading:20674358-CHO Cells,
pubmed-meshheading:20674358-Cricetinae,
pubmed-meshheading:20674358-Cricetulus,
pubmed-meshheading:20674358-Drug Discovery,
pubmed-meshheading:20674358-Pyrrolidines,
pubmed-meshheading:20674358-Receptors, CCR5,
pubmed-meshheading:20674358-Stereoisomerism,
pubmed-meshheading:20674358-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
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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pubmed:affiliation |
Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, PR China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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