Selective PPARgamma modulators with improved pharmacological profiles.

Kun Liu; Regina M Black; John J Acton; Ralph Mosley; Sheryl Debenham; Ramon Abola; Meng Yang; Richard Tschirret-Guth; Lawrence Colwell; Cherrie Liu; Margaret Wu; Chuanlin F Wang; Karen L MacNaul; Margaret E McCann; David E Moller; Joel P Berger; Peter T Meinke; A Brian Jones; Harold B Wood

doi:10.1016/j.bmcl.2005.03.092

PubMed · 15863293

Selective PPARgamma modulators with improved pharmacological profiles.

Kun Liu·Regina M Black·John J Acton·Ralph Mosley·Sheryl Debenham·Ramon Abola·Meng Yang·Richard Tschirret-Guth·Lawrence Colwell·Cherrie Liu·Margaret Wu·Chuanlin F Wang·Karen L MacNaul·Margaret E McCann·David E Moller·Joel P Berger·Peter T Meinke·A Brian Jones·Harold B Wood

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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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Animals Area Under Curve Blood Glucose Humans Indoles Mice PPAR gamma Rats Journal Article

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Kun Liu, Regina M Black, John J Acton, Ralph Mosley, Sheryl Debenham, Ramon Abola, Meng Yang, Richard Tschirret-Guth, Lawrence Colwell, Cherrie Liu, Margaret Wu, Chuanlin F Wang, Karen L MacNaul, Margaret E McCann, David E Moller, Joel P Berger, Peter T Meinke, A Brian Jones, Harold B Wood. 2005-05-16. Selective PPARgamma modulators with improved pharmacological profiles.. https://doi.org/10.1016/j.bmcl.2005.03.092

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