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Comparative Study
. 2005 Jan 17;15(2):357-62.
doi: 10.1016/j.bmcl.2004.10.068.

Benzoyl 2-methyl indoles as selective PPARgamma modulators

John J Acton 3rd  1 , Regina M Black, A Brian Jones, David E Moller, Lawrence Colwell, Thomas W Doebber, Karen L Macnaul, Joel Berger, Harold B Wood
Affiliations
Comparative Study

Benzoyl 2-methyl indoles as selective PPARgamma modulators

John J Acton 3rd et al. Bioorg Med Chem Lett. .

Abstract

Routine screening for human PPAR ligands yielded compounds 1 and 2, both of which were sub-micromolar hPPARgamma 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 PPARgamma modulators (SPPARgammaMs). SPPARgammaM 24 displayed robust anti-diabetic activity with an improved therapeutic window in comparison to a PPARgamma full agonist in a rodent efficacy model.

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