Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 8, 2014, Pages 1934-1940

  Razavi, Hossein ^a   Riether, Doris ^a   Harcken, Christian ^a   Bentzien, Jörg ^a   Dinallo, Roger M ^a   Souza, Donald ^a   Nelson, Richard M ^a   Kukulka, Alison ^a   Fadra Khan, Tazmeen N ^a   Pack, Edward J ^a   Zuvela Jelaska, Ljiljana ^a   Pelletier, Josephine ^a   Panzenbeck, Mark ^a   Torcellini, Carol A ^a   Proudfoot, John R ^a   Nabozny, Gerald H ^a   Thomson, David S ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

Author keywords

Agonist; Dissociated; Glucocorticoids; Non steroidal; Nuclear hormone receptors

Indexed keywords

DEXAMETHASONE; FATTY ACID; HORMONE RECEPTOR STIMULATING AGENT; INSULIN; INTERLEUKIN 6; METHANOL DERIVATIVE; MINERALOCORTICOID RECEPTOR; NONSTEROID ANTIINFLAMMATORY AGENT; PREDNISOLONE; PROGESTERONE RECEPTOR; TRIACYLGLYCEROL;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ARTHRITIS; ARTICLE; BODY FAT; CONTROLLED STUDY; CRYSTAL STRUCTURE; DISSOCIATION; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SOLUBILITY; DRUG SYNTHESIS; FEMALE; HORMONE RECEPTOR INTERACTION; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MEAN RESIDENCE TIME; MOLECULAR DOCKING; MOUSE; MOUSE MODEL; NONHUMAN; PHARMACOPHORE; RAT; STRUCTURE ACTIVITY RELATION; TOXICITY TESTING; TRANSCRIPTION INITIATION; WEIGHT CHANGE;

MOUSE MAMMARY TUMOR VIRUS;

AGONIST; DISSOCIATED; GLUCOCORTICOIDS; NON-STEROIDAL; NUCLEAR HORMONE RECEPTORS;

ANIMALS; ANTI-INFLAMMATORY AGENTS; ARTHRITIS; BINDING SITES; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; GLUCOCORTICOIDS; HUMANS; INHIBITORY CONCENTRATION 50; METHANOL; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PREDNISOLONE; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GLUCOCORTICOID;

EID: 84897538777     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.03.005     Document Type: Article

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