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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2008-3-17
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pubmed:abstractText |
Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38alpha MAP kinase are described. The issue of metabolic instability associated with vicinal phenyl, benzo[d]thiazol-6-yl oxazoles/imidazoles was addressed by the replacement of the central oxazole or imidazole ring with an aminopyrazole system. The proposed binding mode of this new class of p38alpha inhibitors was confirmed by X-ray crystallographic studies of a representative inhibitor (6a) bound to the p38alpha enzyme.
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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 |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BarrishJoel CJC,
pubmed-author:DoddJohn HJH,
pubmed-author:DoweykoArthur MAM,
pubmed-author:KieferSusan ESE,
pubmed-author:KishKevinK,
pubmed-author:LeftherisKaterinaK,
pubmed-author:LinJamesJ,
pubmed-author:LiuChunjianC,
pubmed-author:MarathePunit HPH,
pubmed-author:MckinnonMurrayM,
pubmed-author:PittSidneyS,
pubmed-author:SackJohn SJS,
pubmed-author:SchievenGary LGL,
pubmed-author:TrzaskosJamesJ,
pubmed-author:ZhangHongjianH,
pubmed-author:ZhangRosemary FRF
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1874-9
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18296051-Animals,
pubmed-meshheading:18296051-Benzothiazoles,
pubmed-meshheading:18296051-Cells, Cultured,
pubmed-meshheading:18296051-Crystallography, X-Ray,
pubmed-meshheading:18296051-Humans,
pubmed-meshheading:18296051-Lipopolysaccharides,
pubmed-meshheading:18296051-Mice,
pubmed-meshheading:18296051-Microsomes,
pubmed-meshheading:18296051-Mitogen-Activated Protein Kinase 14,
pubmed-meshheading:18296051-Molecular Structure,
pubmed-meshheading:18296051-Protein Kinase Inhibitors,
pubmed-meshheading:18296051-Rats,
pubmed-meshheading:18296051-Structure-Activity Relationship,
pubmed-meshheading:18296051-Tumor Necrosis Factor-alpha
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pubmed:year |
2008
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pubmed:articleTitle |
Benzothiazole based inhibitors of p38alpha MAP kinase.
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pubmed:affiliation |
Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543-4000, USA. chunjian.liu@bms.com
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pubmed:publicationType |
Journal Article
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