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.
Keywords: 2-Azetidinones, C-3 sidechain, Cholesterol absorption inhibition activity
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