Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.

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Humphries PS, Bailey S, Almaden JV, Barnum SJ, Carlson TJ, Christie LC, Do QQ, Fraser JD, Hess M, Kellum J, Kim YH, McClellan GA, Ogilvie KM, Simmons BH, Skalitzky D, Sun S, Wilhite D, Zehnder LR

Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6120-3. Epub 2006 Sep 14.

PubMed ID
16973358 [ View in PubMed
]
Abstract

A series of novel pyridine-3-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, compounds (S)-14 and (S)-19 were 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 alphaEC 50 (nM)3000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)158N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaKi (nM)440N/AN/ADetails