4-CF3-ezetimibe analogs: design, synthesis, and biological evaluation of cholesterol absorption inhibitions
文献类型：期刊论文
| 作者 | Liu, Yingle1; Chen, Jun-Ling1; Wang, Gai-Hong3; Sun, Peng3; Huang, Heyao3; Qing, Feng-Ling1,2 |
| 刊名 | TETRAHEDRON LETTERS
 |
| 出版日期 | 2013-10-02 |
| 卷号 | 54期号:40页码:5541-5543 |
| 关键词 | Ezetimibe Cholesterol beta-Lactam Trifluoromethyl Asymmetric hydrogention |
| ISSN号 | 0040-4039 |
| DOI | 10.1016/j.tetlet.2013.08.027 |
| 文献子类 | Article |
| 英文摘要 | On the purpose of looking for better cholesterol absorption inhibitors, several trifluoromethyl substituted ezetimibe analogs 1a-d were designed and synthesized. The key steps in the synthesis of these optically pure trans-4-CF3-beta-lactams include chiral auxiliary induced asymmetric hydrogenation and substrate controlled stereoselective alkylation. The inhibitory activities of these target compounds were evaluated on the cholesterol absorption in Caco-2 cells. The result showed that the inhibitory activity of compound 1a was comparable to ezetimibe. (C) 2013 Elsevier Ltd. All rights reserved. |
| WOS关键词 | BETA-AMINO-ACIDS ; STEREOSELECTIVE-SYNTHESIS ; MEDICINAL CHEMISTRY ; EZETIMIBE ; DERIVATIVES ; CONVENIENT ; DISCOVERY ; FLUORINE ; RING ; CYCLIZATION |
| 资助项目 | National Natural Science Foundation of China[21072028] ; National Natural Science Foundation of China[21272036] ; National Basic Research Program of China[2012CB21600] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000324452100030 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277427]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Qing, Feng-Ling |
| 作者单位 | 1.Donghua Univ, Coll Chem Chem Engn & Biotechnol, Shanghai 201620, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, Shanghai 200032, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Yingle,Chen, Jun-Ling,Wang, Gai-Hong,et al. 4-CF3-ezetimibe analogs: design, synthesis, and biological evaluation of cholesterol absorption inhibitions[J]. TETRAHEDRON LETTERS,2013,54(40):5541-5543. |
| APA | Liu, Yingle,Chen, Jun-Ling,Wang, Gai-Hong,Sun, Peng,Huang, Heyao,&Qing, Feng-Ling.(2013).4-CF3-ezetimibe analogs: design, synthesis, and biological evaluation of cholesterol absorption inhibitions.TETRAHEDRON LETTERS,54(40),5541-5543. |
| MLA | Liu, Yingle,et al."4-CF3-ezetimibe analogs: design, synthesis, and biological evaluation of cholesterol absorption inhibitions".TETRAHEDRON LETTERS 54.40(2013):5541-5543. |
入库方式： OAI收割
来源：上海药物研究所
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