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

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor gammaIC 50 (nM)210N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)22N/AN/ADetails