Selective PPARgamma modulators with improved pharmacological profiles.

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Liu K, Black RM, Acton JJ 3rd, Mosley R, Debenham S, Abola R, Yang M, Tschirret-Guth R, Colwell L, Liu C, Wu M, Wang CF, MacNaul KL, McCann ME, Moller DE, Berger JP, Meinke PT, Jones AB, Wood HB

Selective PPARgamma modulators with improved pharmacological profiles.

Bioorg Med Chem Lett. 2005 May 16;15(10):2437-40.

PubMed ID

15863293 [ View in PubMed

]

Abstract

A series of metabolically robust N-benzyl-indole selective PPARgamma modulators with either a 3-benzoyl or 3-benzisoxazoyl moiety have been identified. In vitro, these compounds are partial agonists and exhibit reduced adipogenesis in human adipocytes. In vivo, these SPPARgammaMs result in potent glucose lowering in db/db mice and attenuate increases in heart weight and brown adipose tissue that is typically observed in rats upon treatment with PPARgamma full agonists.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	20	N/A	N/A	Details
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	IC 50 (nM)	250	N/A	N/A	Details