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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2010-8-24
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pubmed:abstractText |
Structural modifications around 8-HETE (8-hydroxyeicosatetraenoic acid), a natural agonist of the PPAR (peroxisome proliferator-activated receptor) nuclear receptors have led previously to the identification of a promising analog, the quinoline S 70655. Series of novel quinoline or benzoquinoline derivatives were designed through the modification of this lead. Variations of the nature of the aromatic core and of the side chains were carried out. The SAR studies indicated the high sensitivity of the upper acid chain to modifications as well as the strong effect of the length and size of the lipophilic side chain. They afforded several new promising PPARalpha/gamma dual agonists with a high PPARalpha activity in vitro.
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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 |
Oct
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pubmed:issn |
1475-6374
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pubmed:author |
pubmed-author:AudinotValérieV,
pubmed-author:AyralErwanE,
pubmed-author:BoutinJean AJA,
pubmed-author:CaignardDaniel HenriDH,
pubmed-author:CaijoFrédéricF,
pubmed-author:DacquetCatherineC,
pubmed-author:GirardAnne-LiseAL,
pubmed-author:GréeRenéR,
pubmed-author:KtorzaAlainA,
pubmed-author:LiutkusMélanieM,
pubmed-author:MossetPaulP,
pubmed-author:RenardPierreP
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pubmed:issnType |
Electronic
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pubmed:volume |
25
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
653-72
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pubmed:meshHeading |
pubmed-meshheading:20518620-Animals,
pubmed-meshheading:20518620-COS Cells,
pubmed-meshheading:20518620-Cercopithecus aethiops,
pubmed-meshheading:20518620-Diabetes Mellitus, Type 2,
pubmed-meshheading:20518620-Drug Design,
pubmed-meshheading:20518620-Genes, Reporter,
pubmed-meshheading:20518620-Humans,
pubmed-meshheading:20518620-Hydroxyeicosatetraenoic Acids,
pubmed-meshheading:20518620-Hypoglycemic Agents,
pubmed-meshheading:20518620-Kinetics,
pubmed-meshheading:20518620-Metabolic Syndrome X,
pubmed-meshheading:20518620-Octanoic Acids,
pubmed-meshheading:20518620-PPAR alpha,
pubmed-meshheading:20518620-PPAR gamma,
pubmed-meshheading:20518620-Peroxisome Proliferator-Activated Receptors,
pubmed-meshheading:20518620-Quinolines,
pubmed-meshheading:20518620-Recombinant Fusion Proteins,
pubmed-meshheading:20518620-Structure-Activity Relationship,
pubmed-meshheading:20518620-Transcriptional Activation
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors.
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pubmed:affiliation |
Université de Rennes 1, Laboratoire de Chimie et Photonique Moléculaires, CNRS UMR 6510, Avenue du Général Leclerc, 35042 Rennes - Cedex, France.
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pubmed:publicationType |
Journal Article
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