| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372819 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
A series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPARγ modulators (SPPARγMs). Addition of substituents at the 6-position of the 7-azaindoles improves in vitro potency and pharmacokinetics. 7-Azaindoles have significantly improved off-target profiles compared to the parent indole series.
Graphical abstractA series of highly functionalized 3-aroyl and 3-phenoxy-2-methyl-7-azaindoles have been identified, which are potent selective PPARγ modulators (SPPARγMs). The SAR around substitution at the 6-position of the azaindole as well as substitution of the N-benzyl moiety is reported. 7-Azaindoles have significantly improved off-target profiles compared to the parent indole series.Figure optionsDownload full-size imageDownload as PowerPoint slide
