Discovery of quinolines as selective glucocorticoid receptor agonists |
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| Authors: | Stefan Jaroch Markus Berger Christoph Huwe Konrad Krolikiewicz Hartmut Rehwinkel Heike Schäcke Norbert Schmees Werner Skuballa |
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| Affiliation: | 1. Medicinal Chemistry Berlin, Lead Generation & Optimization, Bayer Schering Pharma AG, Berlin D-13342, Germany;2. Common Mechanism Research Berlin, Global Therapeutic Research, Bayer Schering Pharma AG, Berlin D-13342, Germany |
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| Abstract: | The dissociated glucocorticoid receptor (GR) agonist ZK 216348 is rendered GR-selective over other nuclear hormone receptors through replacing the methylbenzoxazine with a quinoline moiety. Compounds were shown to be efficacious in cell assays with respect to inflammation endpoints, along with reduced activity in a transactivation assay, hinting at an improved therapeutic window over corticosteroids. |
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