| Literature DB >> 15603954 |
John J Acton1, Regina M Black, A Brian Jones, David E Moller, Lawrence Colwell, Thomas W Doebber, Karen L Macnaul, Joel Berger, Harold B Wood.
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.Entities:
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Year: 2005 PMID： 15603954 DOI： 10.1016/j.bmcl.2004.10.068
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823