Abstract
Sequential, position-selective, Pd-catalyzed cross-coupling reactions of 2,4-dibromo-5-hydroxymethylthiazole provided the scaffold for the synthesis of GW501516, the most potent PPARbeta/delta agonist yet described, and equally selective analogs at the thiazole-C4 position.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Catalysis
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Cell Line
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Chemistry, Pharmaceutical
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Drug Design
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Genes, Reporter
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Genetic Techniques
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Globins / genetics
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HeLa Cells
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Humans
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Hydroxybenzoates / chemistry*
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Ligands
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Lipids / chemistry
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Models, Chemical
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PPAR delta / agonists*
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PPAR-beta / agonists*
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Palladium / pharmacology
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Promoter Regions, Genetic
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Quinazolines / chemical synthesis*
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Quinazolines / pharmacology
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Thiazoles / chemical synthesis
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Thiazoles / chemistry*
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Thiazoles / pharmacology
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Time Factors
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Transcription, Genetic
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Transcriptional Activation
Substances
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CB676475
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GW 501516
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Hydroxybenzoates
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Ligands
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Lipids
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PPAR delta
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PPAR-beta
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Quinazolines
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Thiazoles
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Palladium
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Globins