Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 15, 2011, Pages 4633-4637

  Dyckman, Alaric J ^a   Li, Tianle ^a   Pitt, Sidney ^a   Zhang, Rosemary ^a   Shen, Ding Ren ^a   McIntyre, Kim W ^a   Gillooly, Kathleen M ^a   Shuster, David J ^a   Doweyko, Arthur M ^a   Sack, John S ^a   Kish, Kevin ^a   Kiefer, Susan E ^a   Newitt, John A ^a   Zhang, Hongjian ^a   Marathe, Punit H ^a   McKinnon, Murray ^a   Barrish, Joel C ^a   Dodd, John H ^a   Schieven, Gary L ^a   Leftheris, Katerina ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Inhibitors; Ketone; MAPK14; p38 MAP kinase; Pyrrolotriazine; Rat adjuvant arthritis model; Structure activity relationships; X ray structure

Indexed keywords

ANTIINFLAMMATORY AGENT; FUSED CARBON NITROGEN HETEROCYCLE; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; TUMOR NECROSIS FACTOR ALPHA;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CHEMICAL MODIFICATION; CHRONIC INFLAMMATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; FEMALE; IN VIVO STUDY; INFLAMMATION; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS; ARTHRITIS; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; FEMALE; MICE; MITOGEN-ACTIVATED PROTEIN KINASE 14; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PYRROLES; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZINES;

RATTUS;

EID: 79960380097     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.05.091     Document Type: Article

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