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rdf:type |
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lifeskim:mentions |
umls-concept:C0066086,
umls-concept:C0132515,
umls-concept:C0205177,
umls-concept:C0243071,
umls-concept:C0243077,
umls-concept:C0376315,
umls-concept:C0680730,
umls-concept:C1148554,
umls-concept:C1565860,
umls-concept:C1705323,
umls-concept:C1883073,
umls-concept:C2603343
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pubmed:issue |
23
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pubmed:dateCreated |
2002-10-31
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pubmed:abstractText |
Compound 7, N-(3-phenoxy-4-pyridinyl)trifluoromethanesulfonamide, showed in vitro (whole blood assay) a strong inhibitory activity on the two cyclooxygenase (COX) enzymes (IC(50)(COX-1) = 2.2 microM and IC(50)(COX-2) = 0.4 microM), being more active but less COX-2-selective than nimesulide. Physicochemical studies and structural analyses indicated that the anionic sulfonamidate species seemed to be the active form of methanesulfonamides, which optimally interacted with the COX enzymes' active sites.
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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/Aminopyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Anions,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Inflammatory Agents...,
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/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/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/nimesulide
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5182-5
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12408728-Aminopyridines,
pubmed-meshheading:12408728-Animals,
pubmed-meshheading:12408728-Anions,
pubmed-meshheading:12408728-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:12408728-Binding Sites,
pubmed-meshheading:12408728-Crystallography, X-Ray,
pubmed-meshheading:12408728-Cyclooxygenase 1,
pubmed-meshheading:12408728-Cyclooxygenase 2,
pubmed-meshheading:12408728-Cyclooxygenase 2 Inhibitors,
pubmed-meshheading:12408728-Cyclooxygenase Inhibitors,
pubmed-meshheading:12408728-Edema,
pubmed-meshheading:12408728-Humans,
pubmed-meshheading:12408728-Isoenzymes,
pubmed-meshheading:12408728-Membrane Proteins,
pubmed-meshheading:12408728-Prostaglandin-Endoperoxide Synthases,
pubmed-meshheading:12408728-Rats,
pubmed-meshheading:12408728-Rats, Wistar,
pubmed-meshheading:12408728-Spectrophotometry, Infrared,
pubmed-meshheading:12408728-Sulfonamides
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pubmed:year |
2002
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pubmed:articleTitle |
Spectral and crystallographic study of pyridinic analogues of nimesulide: determination of the active form of methanesulfonamides as COX-2 selective inhibitors.
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pubmed:affiliation |
Natural and Synthetic Drugs Research Center, Department of Medicinal Chemistry, Université de Liège, 1, Avenue de l'Hôpital, Tour 4(+5) Sart-Tilman, Belgium. f.julemont@ulg.ac.be
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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