Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors

A series of saucerneol B derivatives 2a-i were prepared for evaluating their acyl-CoA: cholesterol acyltransferase inhibitory activities. Compounds 2a-g showed more specificity of hACAT-1 than hACAT-2. Saucerneol B (1) exhibited strong cholesterol-lowering effect in high cholesterol-fed mice.