Title of article
Benzoyl 2-methyl indoles as selective PPARγ modulators
Author/Authors
John J. Acton III، نويسنده , , Regina M. Black، نويسنده , , A. Brian Jones، نويسنده , , David E. Moller، نويسنده , , Lawrence Colwell، نويسنده , , Thomas W. Doebber، نويسنده , , Karen L. MacNaul، نويسنده , , Joel Berger، نويسنده , , Harold B. Wood، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
357
To page
362
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 efficacy model.
Keywords
PPAR , Indole , Selective PPAR modulator
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795207
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