- Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Bioorganic & medicinal chemistry letters (2005-09-13)
James F Dropinski, Taro Akiyama, Monica Einstein, Bahanu Habulihaz, Tom Doebber, Joel P Berger, Peter T Meinke, Guo Q Shi
PMID16153845
摘要
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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