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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2002-10-23
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pubmed:abstractText |
The COX-2 inhibitor DFP [5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone] was found to have a long half-life in humans. Analogues have been characterized in order to optimize pharmacokinetics. This has lead to the discovery of 5(S)-(5-ethyl-5-methyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone analogue 11 a potent and selective COX-2 inhibitor which is metabolized to a greater extent than DFP upon incubation with rat and human hepatocytes, suggesting a shorter half-life in humans.
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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/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/Indomethacin,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Lactones,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/PTGS2 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin-Endoperoxide Synthases,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfones,
http://linkedlifedata.com/resource/pubmed/chemical/rofecoxib
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AubinYvesY,
pubmed-author:BrideauChristineC,
pubmed-author:ChanChi ChungCC,
pubmed-author:ChauretNathalieN,
pubmed-author:GordonRobertR,
pubmed-author:LeblancYvesY,
pubmed-author:LiChun SingCS,
pubmed-author:Nicoll-GriffithDeborah ADA,
pubmed-author:PrasitPetpiboonP,
pubmed-author:RiendeauDenisD,
pubmed-author:RoyPatrickP,
pubmed-author:SilvaJosé MJM,
pubmed-author:ViscoDenise MDM,
pubmed-author:WangZhaoyinZ,
pubmed-author:WebbJanineJ,
pubmed-author:XuLijingL,
pubmed-author:YergeyJames AJA
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pubmed:issnType |
Print
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pubmed:day |
18
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3317-20
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12392741-Animals,
pubmed-meshheading:12392741-Cyclooxygenase 2,
pubmed-meshheading:12392741-Cyclooxygenase 2 Inhibitors,
pubmed-meshheading:12392741-Cyclooxygenase Inhibitors,
pubmed-meshheading:12392741-Dose-Response Relationship, Drug,
pubmed-meshheading:12392741-Drug Evaluation, Preclinical,
pubmed-meshheading:12392741-Hepatocytes,
pubmed-meshheading:12392741-Humans,
pubmed-meshheading:12392741-Indomethacin,
pubmed-meshheading:12392741-Inhibitory Concentration 50,
pubmed-meshheading:12392741-Isoenzymes,
pubmed-meshheading:12392741-Lactones,
pubmed-meshheading:12392741-Membrane Proteins,
pubmed-meshheading:12392741-Pharmacokinetics,
pubmed-meshheading:12392741-Prostaglandin-Endoperoxide Synthases,
pubmed-meshheading:12392741-Rats,
pubmed-meshheading:12392741-Structure-Activity Relationship,
pubmed-meshheading:12392741-Sulfones
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pubmed:year |
2002
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pubmed:articleTitle |
Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Quebec, Canada. yves_leblanc@merck.com
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pubmed:publicationType |
Journal Article,
Comparative Study
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