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Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists
Authors:Dropinski James F  Akiyama Taro  Einstein Monica  Habulihaz Bahanu  Doebber Tom  Berger Joel P  Meinke Peter T  Shi Guo Q
Institution:Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. James_Dropinski@merck.com
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.
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