Sixteen 2-azetidinones were designed and synthesized as cholesterol absorption inhibitors. The length of C-3 side chain was modified to four atoms by introducing ester or amide linkage to investigate further structure-activity relationships. The target compounds exhibited different cholesterol absorption inhibition activities, some of which were promising.
Keywords: 2-Azetidinone, Cholesterol absorption inhibitor, NPC1L1, Ezetimibe, Bioactivities, Structure-activity relationship
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