Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARγ partial agonists

A series of novel aryl indole-2-carboxylic acids has been identified as potent selective PPARγ 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.

A series of novel aryl indole-2-carboxylic acids has been identified as potent selective PPARγ modulators. Their chemical synthesis and in vitro activities are discussed. An optimized compound was efficacious in the db/db mouse model of type 2 diabetes.Figure optionsDownload as PowerPoint slide