Bioactivation of 2-Acyl-5-chlorothiophene-containing Compounds by Human Liver Microsomes

摘要

Background subtraction of LC/accurate MS data is a very sensitive, unbiased methodology for the detection of GSH adducts. The 5-chloro-substitution of thiophenes does not completely block the bioactivation as evidenced by the formation of glutathione adducts from most of the 5-chlorothiophenes. The introduction of alkyl substitutions on the C5 position may be the best to reduce the bioactivation potential of thiophene-containing compounds.