p38 MAP kinase inhibitors. Part 5: Discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 20, 2006, Pages 5468-5471

  Natarajan, Swaminathan R ^a   Liu, Luping ^a   Levorse, Mark ^a   Thompson, James E ^a   O'Neill, Edward A ^a   O'Keefe, Stephen J ^a   Vora, Kalpit A ^a   Cvetovich, Raymond ^a   Chung, John Y ^a   Carballo Jane, Ester ^a   Visco, Denise M ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

7 Amino naphthyridones; p38 MAP kinase inhibitors; Peptide flip; Rat LPS challenge

Indexed keywords

5 (2,6 DICHLOROPHENYL) 2 (2,4 DIFLUOROPHENYLTHIO)PYRIMIDO[1,6 B]PYRIDAZIN 6 ONE; 7 AMINONAPHTHYRIDONE DERIVATIVE; AMINOPYRIDINE DERIVATIVE; LIPOPOLYSACCHARIDE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE P38; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; ENZYME LINKED IMMUNOSORBENT ASSAY; FEMALE; IN VITRO STUDY; INFLAMMATION; LIVER MICROSOME; MONOCYTE; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BINDING SITES; BIOLOGICAL AVAILABILITY; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME ACTIVATION; ENZYME INHIBITORS; HUMANS; LIPOPOLYSACCHARIDES; MACACA MULATTA; MALE; MICE; MICE, INBRED BALB C; MICROSOMES, LIVER; MOLECULAR STRUCTURE; MONOCYTES; NAPHTHYRIDINES; P38 MITOGEN-ACTIVATED PROTEIN KINASES; RATS; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR NECROSIS FACTOR-ALPHA;

ANIMALIA;

EID: 33748311962     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.06.084     Document Type: Article

References (7)

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