Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.

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Humphries PS, Almaden JV, Barnum SJ, Carlson TJ, Do QQ, Fraser JD, Hess M, Kim YH, Ogilvie KM, Sun S

Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6116-9. Epub 2006 Sep 18.

PubMed ID
16979341 [ View in PubMed
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Abstract

A series of novel pyridine-2-propanoic acids was synthesized. A structure-activity relationship study of these compounds led to the identification of potent dual PPARalpha/gamma agonists with varied isoform selectivity. Based on the results of efficacy studies in diabetic (db/db) mice, and the desired pharmacokinetic parameters, compound (S)-13 was selected for further profiling.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)158N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaKi (nM)440N/AN/ADetails