1,3-DISUBSTITUTED UREAS AS ACAT INHIBITORS, AND METHOD OF PREPARING THEREOF

摘要

The invention relates to 1,3-disubstituted ureas of general formula (I) where R<1> is an aryl, R<2> is nitro and/or amino, and X is oxygen and/or sulfur, and the method of preparing thereof which consists in treating aromatic amines with isocyanates. Isocyanates may be formed in situ and the reaction carried out in toluene, at 80 DEG C. If the nitro group is formed, it is reduced with hydrogen in the presence of palladium catalyst to the amino group. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co-enzyme A: cholesterol acyltransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.