Abstract
A series of novel aryl indole-2-carboxylic acids has been identified as potent selective PPARgamma modulators. Their chemical synthesis and in vitro activities are discussed. Compound 5 was selected for in vivo testing in the db/db mouse model of type 2 diabetes and resulted in reduction of hyperglycemia at comparable plasma exposure when compared to rosiglitazone.
MeSH terms
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Animals
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Blood Glucose / metabolism
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Carboxylic Acids
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Disease Models, Animal
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology*
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Inhibitory Concentration 50
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Male
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Mice
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Molecular Structure
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PPAR gamma / agonists*
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PPAR gamma / metabolism
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Structure-Activity Relationship
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Titrimetry
Substances
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Blood Glucose
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Carboxylic Acids
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Indoles
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PPAR gamma
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indole-2-carboxylic acid