5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.

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Koyama H, Boueres JK, Han W, Metzger EJ, Bergman JP, Gratale DF, Miller DJ, Tolman RL, MacNaul KL, Berger JP, Doebber TW, Leung K, Moller DE, Heck JV, Sahoo SP

5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.

Bioorg Med Chem Lett. 2003 May 19;13(10):1801-4.

PubMed ID
12729668 [ View in PubMed
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Abstract

A series of 5-aryl thiazolidine-2,4-diones containing 4-phenoxyphenyl side chains was designed, synthesized, and evaluated for PPAR agonist activities. One such compound 28 exhibited comparable levels of glucose correction to rosiglitazone in the db/db mouse type 2 diabetes animal model.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor alphaIC 50 (nM)>50000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)>3000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor deltaIC 50 (nM)>50000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor deltaEC 50 (nM)>3000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)20N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaIC 50 (nM)250N/AN/ADetails