Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors

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.

Cite this article as:

Ji Jianfeng, Zhao Rui, Huang Wenlong, Zhang Huibin, Zhou Jinpei, Wang Yubin and Qian Hai, Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors, Letters in Drug Design & Discovery 2009; 6 (6) . https://dx.doi.org/10.2174/157018009789057562