Pharmacophore-based design, synthesis, and biological evaluation of novel 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides as cholesteryl ester transfer protein (CETP) inhibitors
文献类型：期刊论文
| 作者 | Zhao DongMei1; Li WenYan1; Shi YuFang2; Xiong XuQiong1; Song Shuai1; Hao ChenZhou1; Cheng MaoSheng1; Shen JingKang2 |
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2014 |
| 卷号 | 25期号:2页码:299-304 |
| 关键词 | CHIRAL N,N-DISUBSTITUTED TRIFLUORO-3-AMINO-2-PROPANOLS POTENT INHIBITORS DISCOVERY TRANSPORT Cholesteryl ester transfer protein CETP inhibitors Pharmacophore Virtual screening Synthesis |
| ISSN号 | 1001-8417 |
| 其他题名 | Pharmacophore-based design, synthesis, and biological evaluation of novel 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides as cholesteryl ester transfer protein (CETP) inhibitors |
| 英文摘要 | Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that plays an important role in decreasing high-density lipoprotein cholesterol (HDL-C) levels and increasing low-density lipoprotein cholesterol (LDL-C) levels. Inhibition of CETP may be a new therapy for treating atherosclerosis. Herein, we report the development of a ligand-based pharmacophore model and pharmacophore-based virtual screening of the ZINC/big-n-greasy database, leading to the identification of compound H-10 as a potential CETP inhibitor in vitro. Based on H-10, a series of 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides were designed, synthesized, and evaluated against CETP. Compound 41 was found to have the best activity, resulting in 85.0% inhibition of CETP at 10 mu mol/L. (C) 2013 Mao-Sheng Cheng and Jing-Kang Shen. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5059654 |
| 源URL | [http://ir.imr.ac.cn/handle/321006/148146]  |
| 专题 | 金属研究所_中国科学院金属研究所 |
| 作者单位 | 1.中国科学院金属研究所 2.Shanghai Pharmaceut Holding Co Ltd, Cent Res Institute, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhao DongMei,Li WenYan,Shi YuFang,et al. Pharmacophore-based design, synthesis, and biological evaluation of novel 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides as cholesteryl ester transfer protein (CETP) inhibitors[J]. CHINESE CHEMICAL LETTERS,2014,25(2):299-304. |
| APA | Zhao DongMei.,Li WenYan.,Shi YuFang.,Xiong XuQiong.,Song Shuai.,...&Shen JingKang.(2014).Pharmacophore-based design, synthesis, and biological evaluation of novel 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides as cholesteryl ester transfer protein (CETP) inhibitors.CHINESE CHEMICAL LETTERS,25(2),299-304. |
| MLA | Zhao DongMei,et al."Pharmacophore-based design, synthesis, and biological evaluation of novel 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides as cholesteryl ester transfer protein (CETP) inhibitors".CHINESE CHEMICAL LETTERS 25.2(2014):299-304. |
入库方式： OAI收割
来源：金属研究所
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