Inhibitors of acyl-CoA: Cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. The synthesis and biological activity of a series of malonester amides

Article abstract of DOI:10.1016/0960-894X(96)00098-4

The synthesis and structure-activity relationships of a series of malonester amide ACAT inhibitors are described. One of these compounds, 4s, was shown to be a potent inhibitor of both the intestinal and arterial enzymes, bioactive upon oral dosing (ex vivo bioassay) and efficacious in a clinically relevant rodent model of preestablished hypercholesterolemia.