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Selective PPARgamma modulators with improved pharmacological profiles |
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| Authors: | Liu Kun Black Regina M Acton John J Mosley Ralph Debenham Sheryl Abola Ramon Yang Meng Tschirret-Guth Richard Colwell Lawrence Liu Cherrie Wu Margaret Wang Chuanlin F MacNaul Karen L McCann Margaret E Moller David E Berger Joel P Meinke Peter T Jones A Brian Wood Harold B |
| Institution: | Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. |
| 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. |
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