National Center for
4CSJ: The Discovery Of Potent Selective Glucocorticoid Receptor Modulators, Suitable For Inhalation
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation
Bioorg. Med. Chem. Lett. (2014) 24 p.2571-2577
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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