Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592159 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
We report the discovery of highly potent and selective non-steroidal glucocorticoid receptor modulators with PK properties suitable for inhalation. A high throughput screen of the AstraZeneca compound collection identified sulfonamide 3 as a potent non-steroidal glucocorticoid receptor ligand. Further optimization of this lead generated indazoles 30 and 48 that were progressed to characterization in in vivo models. X-ray crystallography was used to gain further insight into the binding mode of selected ligands.
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Authors
Karl Edman, Ragnhild Ahlgren, Malena Bengtsson, HÃ¥kan Bladh, Stefan Bäckström, Jan Dahmén, Krister Henriksson, Per Hillertz, Vijakumar Hulikal, Anders Jerre, Liz Kinchin, Charlotte KÃ¥se, Matti Lepistö, Irene Mile, Stinabritt Nilsson,