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
Letters in Drug Design & Discovery
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.
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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
DOI https://dx.doi.org/10.2174/157018009789057562 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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