Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Article Details
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Dropinski JF, Akiyama T, Einstein M, Habulihaz B, Doebber T, Berger JP, Meinke PT, Shi GQ
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
Bioorg Med Chem Lett. 2005 Nov 15;15(22):5035-8.
- PubMed ID
- 16153845 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor gamma IC 50 (nM) 210 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 22 N/A N/A Details