Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.

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Lamotte Y, Martres P, Faucher N, Laroze A, Grillot D, Ancellin N, Saintillan Y, Beneton V, Gampe RT Jr

Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1399-404. doi: 10.1016/j.bmcl.2009.12.107. Epub 2010 Jan 4.

PubMed ID
20079636 [ View in PubMed
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Abstract

Starting from the structure of Telmisartan, a new series of potent and selective PPARgamma modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds are reported and the X-ray structure of compound 7b bound to the PPARgamma ligand binding domain is described.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TelmisartanPeroxisome proliferator-activated receptor gammaIC 50 (nM)12200N/AN/ADetails
TelmisartanPeroxisome proliferator-activated receptor gammaEC 50 (nM)2020N/AN/ADetails
TelmisartanType-1 angiotensin II receptorIC 50 (nM)3N/AN/ADetails