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Bioorg Med Chem Lett. 2005 Jan 17;15(2):357-62.

Benzoyl 2-methyl indoles as selective PPARgamma modulators.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. john_acton@merck.com

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.

PMID:
15603954
DOI:
10.1016/j.bmcl.2004.10.068
[Indexed for MEDLINE]

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