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Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists |
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| Authors: | Hudson Andrew R Higuchi Robert I Roach Steven L Adams Mark E Vassar Angela Syka Peter M Mais Dale E Miner Jeffrey N Marschke Keith B Zhi Lin |
| Affiliation: | Discovery Research, Ligand Pharmaceuticals, 11085 North Torrey Pines Road, Suite 300, La Jolla, CA 92037, USA |
| Abstract: | A series of tetrahydroquinoline derivatives were synthesized and profiled for their ability to act as glucocorticoid receptor selective modulators. Structure-activity relationships of the tetrahydroquinoline B-ring lead to the discovery of orally available GR-selective agonists with high in vivo activity. |
| Keywords: | Glucocorticoid SGRM SEGRA Hormone Tetrahydroquinoline Prednisolone Dexamethasone |
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