Benzothiazole based inhibitors of p38α MAP kinase

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 6, 2008, Pages 1874-1879

  Liu, Chunjian ^a   Lin, James ^a   Pitt, Sidney ^a   Zhang, Rosemary F ^a   Sack, John S ^a   Kiefer, Susan E ^a   Kish, Kevin ^a   Doweyko, Arthur M ^a   Zhang, Hongjian ^a   Marathe, Punit H ^a   Trzaskos, James ^a   Mckinnon, Murray ^a   Dodd, John H ^a   Barrish, Joel C ^a   Schieven, Gary L ^a   Leftheris, Katerina ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

benzo d thiazol 6 yl imidazoles; benzo d thiazol 6 yl oxazoles; benzo d thiazol 6 yl pyrazoles; Benzothiazoles; Inhibitors of p38 MAP kinase; TNF inhibition in hPBMC; Vicinal phenyl; X ray co crystal structure

Indexed keywords

4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; AMINOPYRAZOLE; BENZO[D]THIAZOL 6 YL IMIDAZOLE DERIVATIVE; BENZO[D]THIAZOL 6 YL OXAZOLE DERIVATIVE; BENZOTHIAZOLE DERIVATIVE; ETANERCEPT; IMIDAZOLE; INFLIXIMAB; MITOGEN ACTIVATED PROTEIN KINASE 14; MITOGEN ACTIVATED PROTEIN KINASE 14 INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; OXAZOLE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG BINDING; DRUG DESIGN; ENZYME INHIBITION; HUMAN; HUMAN CELL; HUMAN TISSUE; INHIBITION KINETICS; METABOLIC REGULATION; NONHUMAN; RAT; X RAY CRYSTALLOGRAPHY;

ANIMALS; BENZOTHIAZOLES; CELLS, CULTURED; CRYSTALLOGRAPHY, X-RAY; HUMANS; LIPOPOLYSACCHARIDES; MICE; MICROSOMES; MITOGEN-ACTIVATED PROTEIN KINASE 14; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR NECROSIS FACTOR-ALPHA;

EID: 40749135810     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.02.011     Document Type: Article

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32. 2EDTA-containing tubes and then centrifuged at 4 °C (1500-2000g) to obtain plasma. Two groups of animals (N = 3 per group) received the compound either as an intravenous infusion (2 mg/kg over 10 min) via the jugular vein or by oral gavage (5 mg/kg). Serial blood samples were obtained at 0.17 (for IV only), 0.25, 0.5, 0.75, 1, 2, 4, 6, and 8 h post dose. Plasma samples, obtained by centrifugation at 4 °C (1500-2000g), were stored at -20 °C until analysis by LC/MS/MS.
33. PDB deposition number: 3C5U.