Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPARgamma partial agonists.

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Furukawa A, Arita T, Fukuzaki T, Satoh S, Mori M, Honda T, Matsui Y, Wakabayashi K, Hayashi S, Araki K, Ohsumi J

Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPARgamma partial agonists.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1348-51. doi: 10.1016/j.bmcl.2011.12.066. Epub 2011 Dec 16.

PubMed ID

22225641 [ View in PubMed

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Abstract

Peroxisome proliferator-activated receptor gamma (PPARgamma) is a potential drug target for treating type 2 diabetes. The selective PPARgamma modulators (SPPARMs), which partially activate the PPARgamma transcriptional activity, are considered to improve the plasma glucose level with attenuated PPARgamma related adverse effects. However, the relationships between desired pharmacological profiles and ligand specific PPARgamma transcriptional profiles have been unclear. And there is also little knowledge of how to control ligand specific PPARgamma transcriptional profiles. Herein, we present synthesis of novel derivatives containing substituent at naphthalene C3 position of compound 1. The novel derivatives showed various maximal efficacies as PPARgamma partial agonist.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	11	N/A	N/A	Details