Title: Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors
Volume: 6
Issue: 6
Author(s): Jianfeng Ji, Rui Zhao, Wenlong Huang, Huibin Zhang, Jinpei Zhou, Yubin Wang and Hai Qian
Affiliation:
Keywords:
2-Azetidinone, Cholesterol absorption inhibitor, NPC1L1, Ezetimibe, Bioactivities, Structure-activity relationship
Abstract: 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.
