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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2009-9-28
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pubmed:abstractText |
The identification and evolution of a series of potent and selective p38 inhibitors is described. p38 inhibitors based on a N-benzyl pyridinone high-throughput screening hit were prepared and their SAR explored. Their design was guided by ligand bound co-crystals of p38alpha. These efforts resulted in the identification of 12r and 19 as orally active inhibitors of p38 with significant efficacy in both acute and chronic models of inflammation.
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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:AlviraEdgardoE,
pubmed-author:BensonAlan GAG,
pubmed-author:Blevis-BalRadhikaR,
pubmed-author:BoehmTerri LTL,
pubmed-author:ChristieLanceL,
pubmed-author:DevadasBalekudruB,
pubmed-author:DevrajRajesh VRV,
pubmed-author:DurleyRichard CRC,
pubmed-author:HepperleMichaelM,
pubmed-author:HickoryBrian SBS,
pubmed-author:HitchcockJeffJ,
pubmed-author:JeromeKevin DKD,
pubmed-author:KurumbailRaviR,
pubmed-author:LiXingX,
pubmed-author:MadsenHeather MHM,
pubmed-author:MarrufoLaura DLD,
pubmed-author:MonahanJoseph BJB,
pubmed-author:NaingWinW,
pubmed-author:OwenTom JTJ,
pubmed-author:PromoMichele AMA,
pubmed-author:RuckerPaul VPV,
pubmed-author:SelnessShaun RSR,
pubmed-author:ShiehHueyH,
pubmed-author:WalkerJohn KJK
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pubmed:issnType |
Electronic
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pubmed:day |
15
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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 |
5851-6
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pubmed:meshHeading |
pubmed-meshheading:19751974-Administration, Oral,
pubmed-meshheading:19751974-Animals,
pubmed-meshheading:19751974-Anti-Inflammatory Agents,
pubmed-meshheading:19751974-Binding Sites,
pubmed-meshheading:19751974-Catalytic Domain,
pubmed-meshheading:19751974-Crystallography, X-Ray,
pubmed-meshheading:19751974-Drug Discovery,
pubmed-meshheading:19751974-Humans,
pubmed-meshheading:19751974-JNK Mitogen-Activated Protein Kinases,
pubmed-meshheading:19751974-Male,
pubmed-meshheading:19751974-Microsomes, Liver,
pubmed-meshheading:19751974-Protein Kinase Inhibitors,
pubmed-meshheading:19751974-Pyridones,
pubmed-meshheading:19751974-Rats,
pubmed-meshheading:19751974-Rats, Sprague-Dawley,
pubmed-meshheading:19751974-Structure-Activity Relationship,
pubmed-meshheading:19751974-p38 Mitogen-Activated Protein Kinases
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pubmed:year |
2009
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pubmed:articleTitle |
Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.
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pubmed:affiliation |
Department of Medicinal Chemistry, Pfizer Corporation, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. shaun.r.selness@pfizer.com
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pubmed:publicationType |
Journal Article
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