Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 6, 2011, Pages 1697-1700

  Hudson, Andrew R ^a   Higuchi, Robert I ^a   Roach, Steven L ^a   Adams, Mark E ^a   Vassar, Angela ^a   Syka, Peter M ^a   Mais, Dale E ^a   Miner, Jeffrey N ^a   Marschke, Keith B ^a   Zhi, Lin ^a  

^a LIGAND PHARMACEUTICALS INC   (United States)

Author keywords

Dexamethasone; Glucocorticoid; Hormone; Prednisolone; SEGRA; SGRM; Tetrahydroquinoline

Indexed keywords

ANTIINFLAMMATORY AGENT; DEXAMETHASONE; GLUCOCORTICOID RECEPTOR; GLUCOCORTICOID RECEPTOR AGONIST; HORMONE RECEPTOR STIMULATING AGENT; PREDNISOLONE; TETRAHYDROQUINOLINE DERIVATIVE; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; CHEMICAL INTERACTION; CHEMICAL MODIFICATION; CHEMICAL REACTION; DERIVATIZATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; IC 50; INFLAMMATION; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; DRUG DISCOVERY; ENZYME-LINKED IMMUNOSORBENT ASSAY; HUMANS; QUINOLINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GLUCOCORTICOID; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79952361840     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.093     Document Type: Article

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