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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2010-11-24
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pubmed:abstractText |
We disclose here a series of P4-benzoxaborole-substituted macrocyclic HCV protease inhibitors. These inhibitors are potent against HCV NS3 protease, their anti-HCV replicon potencies are largely impacted by substitutions on benzoxaborole ring system and P2? groups. P2? 2-thiazole-isoquinoline provides best replicon potency. The in vitro SAR studies and in vivo PK evaluations of selected compounds are described herein.
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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 |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BakerStephen JSJ,
pubmed-author:CrosbyRenae MRM,
pubmed-author:DingCharles ZCZ,
pubmed-author:DuanMaoshengM,
pubmed-author:JarvestRichard LRL,
pubmed-author:JiJingjingJ,
pubmed-author:KazmierskiWieslaw MWM,
pubmed-author:LiXianfengX,
pubmed-author:LiuLiangL,
pubmed-author:NiZhi-JieZJ,
pubmed-author:PlattnerJacob JJJ,
pubmed-author:SmithGary KGK,
pubmed-author:TallantMatthew DMD,
pubmed-author:VoasRR,
pubmed-author:WangAmy AAA,
pubmed-author:WrightJonJ,
pubmed-author:WrightLois LLL,
pubmed-author:ZhangSuomingS,
pubmed-author:ZhangYong-KangYK,
pubmed-author:ZhouYasheenY,
pubmed-author:ZouWuxinW
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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 |
15
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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 |
7317-22
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pubmed:meshHeading |
pubmed-meshheading:21067923-Administration, Oral,
pubmed-meshheading:21067923-Animals,
pubmed-meshheading:21067923-Antiviral Agents,
pubmed-meshheading:21067923-Hepacivirus,
pubmed-meshheading:21067923-Isoquinolines,
pubmed-meshheading:21067923-Macrocyclic Compounds,
pubmed-meshheading:21067923-Protease Inhibitors,
pubmed-meshheading:21067923-Rats,
pubmed-meshheading:21067923-Structure-Activity Relationship,
pubmed-meshheading:21067923-Thiazoles,
pubmed-meshheading:21067923-Viral Nonstructural Proteins
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease.
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pubmed:affiliation |
Anacor Pharmaceuticals, Inc., Palo Alto, CA 94303, USA. charles.ding@gmail.com
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pubmed:publicationType |
Journal Article
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