Design and Synthesis of 2-Azetidinone Cholesterol Absorption Inhibitors

In this paper we reported the design, synthesis of a series 2-azetidinones with ester or amide group in C-3 sidechain. Their cholesterol absorption inhibition activity was assessed in orally dosed, cholesterol-fed hamsters. It was demonstrated that compound 20c∼d with amid group in C-3 sidechain exhibited high cholesterol absorption inhibition activity.