Development of a new class of benzoylpyrrole-based PPARalpha/gamma activators.

Article Details

Citation

Ushiroda K, Maruta K, Kitoh M, Iwai K, Nagamine J, Tsuchida A, Taiji M, Nagata R

Development of a new class of benzoylpyrrole-based PPARalpha/gamma activators.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):220-4. doi: 10.1016/j.bmcl.2010.11.032. Epub 2010 Nov 12.

PubMed ID
21130649 [ View in PubMed
]
Abstract

Starting with a subtle blood glucose-lowering effect of a TGF-beta inhibitor, we designed and synthesized a series of benzoylpyrrole-based carboxylic acids as PPARs activators. Among these compounds, 10sNa exhibited favorable blood glucose-lowering effect without body weight gain. We assume that the beneficial effect of 10sNa is attributed to not only its compound PPARalpha agonistic activity but also its PPARgamma partial agonistic activity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PioglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)390N/AN/ADetails