The metabolic activation of (S)-5,6-difluoro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone, DPC 963, in rats was investigated by identifying and characterizing the GSH and mercapturic acid conjugates excreted in the bile and urine, respectively. The structures of these adducts, which were unequivocally elucidated by LC/MS/MS and NMR experiments, revealed the existence o...