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]
- 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
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) >10000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 158 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma Ki (nM) 440 N/A N/A Details