N-Hydroxyglycine derivatives as novel inhibitors of squalene synthase

The squalene synthase inhibiting properties of farnesyl diphosphate (FPP) mimics, 3 and related analogues, are described. The results indicate that the nonphosphorus-containing N-hydroxyglycine is a novel replacement for the diphosphate group. Further optimization of 3 has led to 12, a new and potent squalene synthase inhibitor.