Synthesis of 3-Ureido Derivatives of Coumarin and 2-Quinolone as Potent Acyl-CoA : Cholesterol Acyltransferase Inhibitors

Novel 3-ureido derivatives of 4-phenylcoumarin and 4-phenyl-2-quinolone were synthesized and evaluated for acyl-CoA : cholesterol acyltransferase (ACAT)-inhibitory activity. These derivatives inhibited rat intestinal ACAT with IC50 values at the 10-8 to 10-9 M level and were found to normalize plasma cholesterol levels in cholesterol-fed rats when administered as dietary admixtures.