Metabolic activation of a pyrazinone-containing thrombin inhibitor. Evidence for novel biotransformation involving pyrazinone ring oxidation, rearrangement, and covalent binding to proteins

Chemical Research in Toxicology

Volumn 16, Issue 2, 2003, Pages 198-207

  Singh, Rominder ^a   Silva Elipe, Maria V ^a   Pearson, Paul G ^a   Arison, Byron H ^a   Wong, Bradley K ^a   White, Rebecca ^a   Yu, Xiao ^a   Burgey, Christopher S ^a   Lin, Jiunn H ^a   Baillie, Thomas A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [3 [[2,2 DIFLUORO 2 (2 PYRIDYL)ETHYL]AMINO] 6 METHYL 2 OXOHYDROPYRAZINYL] N [3 FLUORO (2 PYRIDYL)METHYL]ACETAMIDE; 6 METHYL 2 OXO 3 AMINOPYRAZINONE; ANTICOAGULANT AGENT; CARBON 14; CYTOCHROME P450; EPOXIDE; GLUTATHIONE; IMIDAZOLE DERIVATIVE; IMINE; PROTEIN; PROTEINASE; PYRAZINE DERIVATIVE; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BIOTRANSFORMATION; COVALENT BOND; DRUG MECHANISM; DRUG STRUCTURE; LIVER MICROSOME; MASS SPECTROMETRY; NONHUMAN; OXIDATION; RADIOACTIVITY; RAT; STOICHIOMETRY;

ADMINISTRATION, ORAL; ANIMALS; BINDING, COMPETITIVE; BIOTRANSFORMATION; CARBON RADIOISOTOPES; EPOXY COMPOUNDS; GLUTATHIONE; HUMANS; IMINES; MICROSOMES, LIVER; NADP; NUCLEAR MAGNETIC RESONANCE, BIOMOLECULAR; OXIDATION-REDUCTION; PROTEASE INHIBITORS; PROTEIN BINDING; PYRAZINES; RATS; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; THROMBIN;

ANIMALIA;

EID: 0037330483     PISSN: 0893228X     EISSN: None     Source Type: Journal    
DOI: 10.1021/tx025635l     Document Type: Article

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