Letters in Drug Design & Discovery

Author(s): Jianfeng Ji, Rui Zhao, Wenlong Huang, Huibin Zhang, Jinpei Zhou, Yubin Wang and Hai Qian

DOI: 10.2174/157018009789057562

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Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors

Page: [424 - 427] Pages: 4

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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.

Keywords: 2-Azetidinone, Cholesterol absorption inhibitor, NPC1L1, Ezetimibe, Bioactivities, Structure-activity relationship