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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
1999-5-20
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pubmed:abstractText |
Cyclopentenones containing a 4-(methylsulfonyl)phenyl group in the 3-position and a phenyl ring in the 2-position are selective inhibitors of cyclooxygenase-2 (COX-2). The selectivity for COX-2 over COX-1 is dramatically improved by substituting the 2-phenyl group with halogens in the meta position or by replacing the phenyl ring with a 2- or 3-pyridyl ring. Thus the 3,5-difluorophenyl derivative 7 (L-776,967) and the 3-pyridyl derivative 13 (L-784,506) are particularly interesting as potential antiinflammatory agents with reduced side-effect profiles. Both exhibit good oral bioavailability and are potent in standard models of pain, fever, and inflammation yet have a much reduced effect on the GI integrity of rats compared to standard nonsteroidal antiflammatory drugs.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Non-Narcotic,
http://linkedlifedata.com/resource/pubmed/chemical/Carrageenan,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 1,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 2,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 2 Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclopentanes,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/PTGS1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/PTGS2 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin-Endoperoxide Synthases,
http://linkedlifedata.com/resource/pubmed/chemical/Ptgs1 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfones
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BlackW CWC,
pubmed-author:BrideauCC,
pubmed-author:ChanC CCC,
pubmed-author:CharlesonSS,
pubmed-author:ChauretNN,
pubmed-author:ClaveauDD,
pubmed-author:EthierDD,
pubmed-author:GordonRR,
pubmed-author:GreifHH,
pubmed-author:GubaAA,
pubmed-author:HughesGG,
pubmed-author:JolicoeurPP,
pubmed-author:LeblancYY,
pubmed-author:Nicoll-GriffithDD,
pubmed-author:OuimetNN,
pubmed-author:PrasitPP,
pubmed-author:RiendeauDD,
pubmed-author:ViscoDD,
pubmed-author:WangZZ,
pubmed-author:YUMM
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pubmed:issnType |
Print
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pubmed:day |
8
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pubmed:volume |
42
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1274-81
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:10197970-Analgesics, Non-Narcotic,
pubmed-meshheading:10197970-Animals,
pubmed-meshheading:10197970-Arthritis, Experimental,
pubmed-meshheading:10197970-Biological Availability,
pubmed-meshheading:10197970-CHO Cells,
pubmed-meshheading:10197970-Carrageenan,
pubmed-meshheading:10197970-Cell Line,
pubmed-meshheading:10197970-Cricetinae,
pubmed-meshheading:10197970-Cyclooxygenase 1,
pubmed-meshheading:10197970-Cyclooxygenase 2,
pubmed-meshheading:10197970-Cyclooxygenase 2 Inhibitors,
pubmed-meshheading:10197970-Cyclooxygenase Inhibitors,
pubmed-meshheading:10197970-Cyclopentanes,
pubmed-meshheading:10197970-Digestive System,
pubmed-meshheading:10197970-Edema,
pubmed-meshheading:10197970-Female,
pubmed-meshheading:10197970-Fever,
pubmed-meshheading:10197970-Humans,
pubmed-meshheading:10197970-Hyperalgesia,
pubmed-meshheading:10197970-Isoenzymes,
pubmed-meshheading:10197970-Male,
pubmed-meshheading:10197970-Membrane Proteins,
pubmed-meshheading:10197970-Microsomes,
pubmed-meshheading:10197970-Prostaglandin-Endoperoxide Synthases,
pubmed-meshheading:10197970-Rats,
pubmed-meshheading:10197970-Rats, Inbred Lew,
pubmed-meshheading:10197970-Rats, Sprague-Dawley,
pubmed-meshheading:10197970-Structure-Activity Relationship,
pubmed-meshheading:10197970-Sulfones,
pubmed-meshheading:10197970-Transfection
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pubmed:year |
1999
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pubmed:articleTitle |
2,3-Diarylcyclopentenones as orally active, highly selective cyclooxygenase-2 inhibitors.
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pubmed:affiliation |
Merck Frosst Centre for Therapeutic Research, P.O. Box 1005, Pointe-Claire-Dorval, Québec, Canada H9R 4P8, and Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.
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pubmed:publicationType |
Journal Article
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