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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2004-7-20
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pubmed:abstractText |
Novel substituted [5,5]-bicyclic pyrzazolones are presented as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. Many of these compounds show low nanomolar activity against lipopolysaccaride (LPS)-induced TNF-alpha production in THP-1 cells. This class of molecules was co-crystallized with mutated p38, and several analogs showed good oral bioavailability in the rat. Oral activity of these compounds in the rat iodoacetate model for osteoarthritis is discussed.
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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 |
Aug
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BooklandRoger GRG,
pubmed-author:BrownKimberly KKK,
pubmed-author:BrugelTodd ATA,
pubmed-author:ClarkMichael PMP,
pubmed-author:DeBiswanathB,
pubmed-author:GolebiowskiAdamA,
pubmed-author:HeitmeyerSandra ASA,
pubmed-author:HsiehLily CLC,
pubmed-author:JanuszMichael JMJ,
pubmed-author:JuergensKarenK,
pubmed-author:LaufersweilerMatthew JMJ,
pubmed-author:LaughlinSteven KSK,
pubmed-author:MekelMarlene JMJ,
pubmed-author:SabatMark PMP,
pubmed-author:TownesJennifer AJA,
pubmed-author:VanRensJohn CJC,
pubmed-author:WalterRichard LRL
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pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4267-72
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pubmed:meshHeading |
pubmed-meshheading:15261284-Administration, Oral,
pubmed-meshheading:15261284-Animals,
pubmed-meshheading:15261284-Biological Availability,
pubmed-meshheading:15261284-Lipopolysaccharides,
pubmed-meshheading:15261284-Models, Molecular,
pubmed-meshheading:15261284-Pyrazolones,
pubmed-meshheading:15261284-Rats,
pubmed-meshheading:15261284-Structure-Activity Relationship,
pubmed-meshheading:15261284-Tumor Necrosis Factor-alpha
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pubmed:year |
2004
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pubmed:articleTitle |
The development of novel inhibitors of tumor necrosis factor-alpha (TNF-alpha) production based on substituted [5,5]-bicyclic pyrazolones.
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pubmed:affiliation |
Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Rd, Mason, OH 45040, USA. laufersweiler.mj@pg.com
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pubmed:publicationType |
Journal Article
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