Bioorganic & Medicinal Chemistry Letters 1984-01-01

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

C Jakobs, L Sweetman, W L Nyhan, S Packman

Index: Bioorg. Med. Chem. Lett. 15(22) , 5035-8, (2005)

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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.