Abstract
We have developed a general solid-phase synthesis for identification of PPAR ligands. Synthesis of a 480-member library led to the identification of a potent PPAR gamma/delta dual agonist 23. Compound 23 showed good plasma exposure in rats and demonstrated antihyperglycemic and antihyperlipidemic efficacy in diabetic fatty Zucker rats.
MeSH terms
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Animals
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DNA-Binding Proteins / agonists*
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Diabetes Mellitus / therapy
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Enzyme Activators / chemical synthesis*
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Enzyme Activators / pharmacology
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Hyperglycemia / prevention & control
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Hyperlipidemias / prevention & control
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Ligands
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Rats
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Rats, Zucker
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Receptors, Cytoplasmic and Nuclear / agonists*
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Transcription Factors / agonists*
Substances
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DNA-Binding Proteins
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Enzyme Activators
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Ligands
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Receptors, Cytoplasmic and Nuclear
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Transcription Factors