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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
19
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pubmed:dateCreated |
2009-9-14
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pubmed:abstractText |
A series of benzo[d]isothiazole-1,1-dioxides were designed and evaluated as inhibitors of HCV polymerase NS5B. Structure-based design led to the incorporation of a high affinity methyl sulfonamide group. Structure-activity relationship (SAR) studies of this series revealed analogues with submicromolar potencies in the HCV replicon assay and moderate pharmacokinetic properties. SAR studies combined with structure based drug design focused on the sulfonamide region led to a novel and potent cyclic analogue.
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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 |
Oct
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AdjabengGeorgeG,
pubmed-author:AlexandrovaLudmilaL,
pubmed-author:Ao-IeongGloriaG,
pubmed-author:BambergJoe TJT,
pubmed-author:BlakeJames FJF,
pubmed-author:BrandlMichaelM,
pubmed-author:BriggsAndrewA,
pubmed-author:ElworthyTodd RTR,
pubmed-author:FarrellRobertR,
pubmed-author:FellJay BJB,
pubmed-author:FischerJohnJ,
pubmed-author:HarrisSeth FSF,
pubmed-author:HendricksRobert TRT,
pubmed-author:HilgenkampRamona KRK,
pubmed-author:LarrabeeSusanS,
pubmed-author:Le PogamSophieS,
pubmed-author:LevequeVincent J PVJ,
pubmed-author:LoyEE,
pubmed-author:MohrPeterP,
pubmed-author:NajeraIsabelI,
pubmed-author:RajyaguruSonalS,
pubmed-author:RobinsonJohn EJE,
pubmed-author:SmithDavid BDB,
pubmed-author:SpencerStacey RSR,
pubmed-author:StengelPeter JPJ,
pubmed-author:SukhtankarSunilS,
pubmed-author:WangBeihanB,
pubmed-author:WongAprilA,
pubmed-author:YeeCalvinC,
pubmed-author:de VicenteJavierJ
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5652-6
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pubmed:meshHeading |
pubmed-meshheading:19709881-Animals,
pubmed-meshheading:19709881-Antiviral Agents,
pubmed-meshheading:19709881-Binding Sites,
pubmed-meshheading:19709881-Crystallography, X-Ray,
pubmed-meshheading:19709881-Haplorhini,
pubmed-meshheading:19709881-Hepacivirus,
pubmed-meshheading:19709881-Rats,
pubmed-meshheading:19709881-Structure-Activity Relationship,
pubmed-meshheading:19709881-Thiazoles,
pubmed-meshheading:19709881-Viral Nonstructural Proteins
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pubmed:year |
2009
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pubmed:articleTitle |
Non-nucleoside inhibitors of HCV polymerase NS5B. Part 4: structure-based design, synthesis, and biological evaluation of benzo[d]isothiazole-1,1-dioxides.
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pubmed:affiliation |
Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. javier.devicente@roche.com
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pubmed:publicationType |
Journal Article
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