Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors

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

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 6 , 2009

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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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Article Details

Year: 2009
Page: [424 - 427]
Pages: 4
DOI: 10.2174/157018009789057562
Price: $65

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