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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
2005-8-18
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pubmed:abstractText |
The design and synthesis of a novel class of 2,3-dihydrobenzofuran-2-carboxylic acids as highly potent and subtype-selective PPARalpha agonists are reported. Systematic study of structure-activity relationships has identified several key structural elements within this class for maintaining the potency and subtype selectivity. Select compounds were evaluated in animal models of dyslipidemia using Syrian hamsters and male Beagle dogs, and all these compounds displayed excellent cholesterol- and triglyceride-lowering activity at dose levels that were much lower than the marketed weak PPARalpha agonist fenofibrate.
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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 |
0022-2623
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pubmed:author |
pubmed-author:AgrawalArunA,
pubmed-author:AlvaroRaulR,
pubmed-author:BergerJoel PJP,
pubmed-author:CaiTian-QuanTQ,
pubmed-author:DropinskiJames FJF,
pubmed-author:HeckJames VJV,
pubmed-author:HernandezMelbaM,
pubmed-author:MacnaulKaren LKL,
pubmed-author:MeinkePeter TPT,
pubmed-author:MollerDavid EDE,
pubmed-author:SahooSoumya PSP,
pubmed-author:SantiniConradC,
pubmed-author:ShiGuo QGQ,
pubmed-author:WrightSamuel DSD,
pubmed-author:ZhangYongY,
pubmed-author:ZhouGaochaoG
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pubmed:issnType |
Print
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pubmed:day |
25
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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 |
5589-99
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:16107159-Animals,
pubmed-meshheading:16107159-Benzofurans,
pubmed-meshheading:16107159-Carboxylic Acids,
pubmed-meshheading:16107159-Cholesterol,
pubmed-meshheading:16107159-Cricetinae,
pubmed-meshheading:16107159-Dogs,
pubmed-meshheading:16107159-Humans,
pubmed-meshheading:16107159-Hyperlipidemias,
pubmed-meshheading:16107159-Hypolipidemic Agents,
pubmed-meshheading:16107159-Male,
pubmed-meshheading:16107159-Mesocricetus,
pubmed-meshheading:16107159-Molecular Conformation,
pubmed-meshheading:16107159-PPAR alpha,
pubmed-meshheading:16107159-Radioligand Assay,
pubmed-meshheading:16107159-Stereoisomerism,
pubmed-meshheading:16107159-Structure-Activity Relationship,
pubmed-meshheading:16107159-Transcriptional Activation,
pubmed-meshheading:16107159-Triglycerides
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pubmed:year |
2005
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pubmed:articleTitle |
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065-0900, USA. guoqiang_shi@merck.com
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pubmed:publicationType |
Journal Article,
In Vitro
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