Synthesis and Bioactivities of 2-Azetidinones as Cholesterol Absorption Inhibitors

被引：1

作者：

Ji, Jianfeng ^{[1
]}

Zhao, Rui ^{[1
]}

Huang, Wenlong ^{[1
]}

Zhang, Huibin ^{[1
]}

Zhou, Jinpei ^{[2
]}

Wang, Yubin ^{[1
]}

Qian, Hai ^{[1
]}

机构：

[1] China Pharmaceut Univ, Ctr Drug Discovery, Nanjing 210009, Peoples R China

[2] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2009年 / 6卷 / 06期

关键词：

2-Azetidinone; Cholesterol absorption inhibitor; NPC1L1; Ezetimibe; Bioactivities; Structure-activity relationship; EZETIMIBE; NPC1L1;

D O I：

10.2174/157018009789057562

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：424 / 427

页数：4

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