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rdf:type |
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lifeskim:mentions |
umls-concept:C0022634,
umls-concept:C0205177,
umls-concept:C0205460,
umls-concept:C0205531,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0226896,
umls-concept:C0387583,
umls-concept:C0442027,
umls-concept:C1527415,
umls-concept:C1883254,
umls-concept:C1999216
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pubmed:issue |
11
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pubmed:dateCreated |
2005-5-26
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pubmed:abstractText |
Incorporation of a spacer group between the central scaffold and the aryl ring resulted in a new cyclooxygenase-2 (COX-2) selective inhibitor core structure, 3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone (20), with COX-2 IC50 = 0.25 microM and COX-1 IC50 = 14 microM (human whole blood assay). Compound 20 was orally active in the rat air pouch model of inflammation, inhibiting white blood cell infiltration and COX-2-derived PG production. Our data support the identification of a novel COX-2 selective inhibitor core structure exemplified by 20.
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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 |
Jun
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AugustyniakMichael EME,
pubmed-author:EarlRichard ARA,
pubmed-author:GarveyDavid SDS,
pubmed-author:JaneroDavid RDR,
pubmed-author:KhanapureSubhash PSP,
pubmed-author:LettsL GordonLG,
pubmed-author:MartinoAllison MAM,
pubmed-author:MurtyMadhavi GMG,
pubmed-author:SchwalbDavid JDJ,
pubmed-author:ShumwayMatthew JMJ,
pubmed-author:TrochaAndrzej MAM,
pubmed-author:YoungDelano VDV,
pubmed-author:ZemtsevaIrina SIS
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pubmed:issnType |
Print
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pubmed:day |
2
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3930-4
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:15916445-Administration, Oral,
pubmed-meshheading:15916445-Animals,
pubmed-meshheading:15916445-Carrageenan,
pubmed-meshheading:15916445-Cyclooxygenase 2,
pubmed-meshheading:15916445-Cyclooxygenase 2 Inhibitors,
pubmed-meshheading:15916445-Cyclooxygenase Inhibitors,
pubmed-meshheading:15916445-Dinoprostone,
pubmed-meshheading:15916445-Inflammation,
pubmed-meshheading:15916445-Male,
pubmed-meshheading:15916445-Prostaglandin-Endoperoxide Synthases,
pubmed-meshheading:15916445-Pyridines,
pubmed-meshheading:15916445-Rats,
pubmed-meshheading:15916445-Rats, Sprague-Dawley,
pubmed-meshheading:15916445-Sulfones
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pubmed:year |
2005
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pubmed:articleTitle |
3-[4-(methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: synthesis and biological evaluation.
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pubmed:affiliation |
NitroMed, Inc., 125 Spring Street, Lexington, Massachusetts 02421, USA. skhanapure@nitromed.com
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pubmed:publicationType |
Journal Article
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