Synthesis and Biological Activity of the Metabolites of Diethyl 4-[(4-Bromo-2-cyanophenyl)carbamoyl]benzylphosphonate (NO-1886)

摘要

Five metabolites of diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate (NO-1886) (1) were synthesized to confirm their proposed structures. The metabolites (2—6) were found to be identical with the synthesized compounds. These metabolites were orally administrated to Triton WR-1339-induced hypertriglyceridemic rats, and the plasma levels of triglycerides were measured to estimate lipoprotcin lipasc activity. All the metabolites showed lower potency than NO-1886.