Synthesis and biological activity of a novel series of indole-derived PPARγ agonists

…, KD Plunket, JA Ray, C Roberson, R Unwalla…

文献索引：Henke, Brad R.; Adkison, Kimberley K.; Blanchard, Steven G.; Leesnitzer, Lisa M.; Mook Jr., Robert A.; Plunket, Kelli D.; Ray, John A.; Roberson, Claudia; Unwalla, Rayomand; Willson, Timothy M. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 23 p. 3329 - 3334

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被引用次数: 44

摘要

The synthesis and structure-activity relationships of a novel series of indole 5-carboxylic acids that bind and activate peroxisome proliferator-activated receptor gamma (PPARγ) are reported. These new analogs are selective for PPARγ vs the other PPAR subtypes, and the most potent compounds in this series are comparable to in vitro potencies at PPARγ reported for the thiazolidinedione-based antidiabetic drugs currently in clinical use. The ...