2. Academic Validation
  3. Benzoyl 2-methyl indoles as selective PPARgamma modulators

Benzoyl 2-methyl indoles as selective PPARgamma modulators

  • Bioorg Med Chem Lett. 2005 Jan 17;15(2):357-62. doi: 10.1016/j.bmcl.2004.10.068.
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

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. john_acton@merck.com
PMID: 15603954 DOI: 10.1016/j.bmcl.2004.10.068
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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