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