Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
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:
Animals, Blood Glucose, Disease Models, Animal, Humans, Indoles, Inhibitory Concentration 50, Male, Mice, Molecular Structure, PPAR gamma, Structure-Activity Relationship, Titrimetry
Animals, Blood Glucose, Disease Models, Animal, Humans, Indoles, Inhibitory Concentration 50, Male, Mice, Molecular Structure, PPAR gamma, Structure-Activity Relationship, Titrimetry
Bioorg Med Chem Lett
Date: Nov. 15, 2005
PubMed ID: 16153845
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