Benzoyl 2-methyl indoles as selective PPARγ modulators

…, L Colwell, TW Doebber, KL MacNaul, J Berger…

Index: Acton III, John J.; Black, Regina M.; Jones, A. Brian; Moller, David E.; Colwell, Lawrence; Doebber, Thomas W.; MacNaul, Karen L.; Berger, Joel; Wood, Harold B. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 2 p. 357 - 362

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Citation Number: 115

Abstract

Routine screening for human PPAR ligands yielded compounds 1 and 2, both of which were sub-micromolar hPPARγ agonists. Synthetic modifications of these leads led to a series of potent substituted 3-benzyl-2-methyl indoles, a subset of which were noted to be selective PPARγ modulators (SPPARγMs). SPPARγM 24 displayed robust anti-diabetic activity with an improved therapeutic window in comparison to a PPARγ full agonist in a rodent ...