A potential dual inhibitor(4) for exogenous absorption and endogenic synthesis of cholesterol was designed based on the conjugation of the β-lactam pharmacophore of ezetimibe and the δ-lactone pharmacophore of statins. The merger of ezetimibe and statin 4 was synthesized from p-hydroxyhenzaldehyde through a ten-step route.1H NMR analysis showed existence of four pairs of enantiomers(5.7:5.7:1:1, molar ratio). And compound 4 was found to lower total glucose(TG) level in rat serum via a high-cholesterol and high-fat feeding experiment.