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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2011-3-14
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pubmed:abstractText |
We have synthesized and evaluated a new series of acyclic P4-benzoxaborole-based HCV NS3 protease inhibitors. Structure-activity relationships were investigated, leading to the identification of compounds 5g and 17 with low nanomolar potency in the enzymatic and cell-based replicon assay. The linker-truncated compound 5j was found to exhibit improved absorption and oral bioavailability in rats, suggesting that further reduction of molecular weight and polar surface area could result in improved drug-like properties of this novel series.
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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 |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BakerStephen JSJ,
pubmed-author:CooperJoel PJP,
pubmed-author:CreechKatrinaK,
pubmed-author:CrosbyRenae MRM,
pubmed-author:DingCharles ZCZ,
pubmed-author:DuanMaoshengM,
pubmed-author:GrimesRichard MRM,
pubmed-author:HUY LYL,
pubmed-author:JarvestRichard LRL,
pubmed-author:JiJing-JingJJ,
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: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 © 2011 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 |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2048-54
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pubmed:meshHeading |
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pubmed:year |
2011
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pubmed:articleTitle |
Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties.
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pubmed:affiliation |
Anacor Pharmaceuticals, Inc, 1020 E Meadow Circle, Palo Alto, CA 94303, USA. xli@anacor.com
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pubmed:publicationType |
Journal Article
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