Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051

The same two major CYP mediated metabolites of DG-051 were produced in the presence of rat, dog, monkey and human liver microsomes. Their respective structures were hypothesized based on mass spectrometry data correlated with the parent structure and confirmed by comparison with authentic synthetic samples. The number of regioisomers synthesized as candidates for metabolite M1 was narrowed down using a metabolic study of a selectively deuterated DG-051 analogue.

The identification and synthesis of two CYP mediated metabolites of DG-051 are reported.Figure optionsDownload as PowerPoint slide