Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 12, 2011, Pages 3823-3827

  Kaptein, Allard ^a   Oubrie, Arthur ^a   De Zwart, Edwin ^a   Hoogenboom, Niels ^a   De Wit, Joeri ^a   Van De Kar, Bas ^a   Van Hoek, Maaike ^a   Vogel, Gerard ^a   De Kimpe, Vera ^a   Schultz Fademrecht, Carsten ^a   Borsboom, Judith ^a   Van Zeeland, Mario ^a   Versteegh, Judith ^a   Kazemier, Bert ^a   De Roos, Jeroen ^a   Wijnands, Frank ^a   Dulos, John ^a   Jaeger, Martin ^a   Leandro Garcia, Paula ^a   Barf, Tjeerd ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Anti TNF ; MAPKAPK2; MK2; Oral bioavailability; Rheumatoid arthritis

Indexed keywords

ADENOSINE TRIPHOSPHATE; HEAT SHOCK PROTEIN 27; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; NITROGEN; PH 089; PIPERIDINE DERIVATIVE; SPIRO 3 PIPERIDYL DERIVATIVE; SPIRO COMPOUND; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CRYSTAL STRUCTURE; CYTOKINE PRODUCTION; DRUG BIOAVAILABILITY; DRUG HALF LIFE; ENZYME ACTIVITY; ENZYME INHIBITION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; LIVER MICROSOME METABOLISM; MOUSE; NONHUMAN; PKA; PROTEIN PHOSPHORYLATION; RAT; STEREOISOMERISM;

ADMINISTRATION, ORAL; ANIMALS; BINDING, COMPETITIVE; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DRUG DISCOVERY; ENZYME ACTIVATION; HUMANS; INHIBITORY CONCENTRATION 50; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; MOLECULAR STRUCTURE; PIPERIDINES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; RATS; SPIRO COMPOUNDS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 79957803610     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.04.016     Document Type: Article

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