Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing two heterocyclic head groups

A series of compounds bearing two heterocyclic substituents were prepared, and evaluated for inhibition of acyl-CoA:cholesterol acyltransferase (ACAT). The heterocyclic groups were chosen for dual potency against hepatic and macrophage cell ACAT. Several examples of ACAT-balanced compounds were discovered, and the results of this study, including synthesis, are presented.