| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370706 | Bioorganic & Medicinal Chemistry Letters | 2015 | 6 Pages |
Abstract
The nuclear receptor RORγ plays a central role in controlling a pro-inflammatory gene expression program in several lymphocyte lineages including TH17 cells. RORγ-dependent inflammation has been implicated in the pathogenesis of several major autoimmune diseases and thus RORγ is an attractive target for therapeutic intervention in these diseases. Starting from a lead biaryl compound 4a, replacement of the head phenyl moiety with a substituted aminopyrazole group resulted in a series with improved physical properties. Further SAR exploration led to analogues (e.g., 4j and 5m) as potent RORγ inverse agonists.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Tao Wang, Daliya Banerjee, Tonika Bohnert, Jianhua Chao, Istvan Enyedy, Jason Fontenot, Kevin Guertin, Howard Jones, Edward Y. Lin, Douglas Marcotte, Tina Talreja, Kurt Van Vloten,