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

…, T Akiyama, M Einstein, B Habulihaz, T Doebber…

文献索引：Dropinski, James F.; Akiyama, Taro; Einstein, Monica; Habulihaz, Bahanu; Doebber, Tom; Berger, Joel P.; Meinke, Peter T.; Shi, Guo Q. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 5035 - 5038

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被引用次数: 52

摘要

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.