کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1372819 | 981882 | 2008 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Highly functionalized 7-azaindoles as selective PPARγ modulators Highly functionalized 7-azaindoles as selective PPARγ modulators](/preview/png/1372819.png)
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.
A 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 as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 17, 1 September 2008, Pages 4798–4801