Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors
文献类型：期刊论文
| 作者 | Liu, Jian2; Chen, Wuyan1; Xu, Yechun1 ; Ren, Sumei2; Zhang, Wei2; Li, Yingxia2
|
| 刊名 | Bioorganic & medicinal chemistry
 |
| 出版日期 | 2015-05-01 |
| 卷号 | 23期号:9页码:1963-74 |
| ISSN号 | 1464-3391 |
| DOI | 10.1016/j.bmc.2015.03.034 |
| 文献子类 | Article |
| 英文摘要 | Nineteen new derivatives based on the structure of marine natural product tasiamide B were designed, synthesized, and evaluated for their inhibitory activity against BACE1, a potential therapeutic target for Alzheimer's disease. The hydrophobic substituents Val at P₃ position, Leu at P₁' position, Ala at P₂' position, and Phe at P₃' position were found to significantly affect the inhibition. Free carboxylic acid at C-terminus was also found to be important to the activity. In addition, the structure-activity relationships (SARs) were supported by molecular docking simulation. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266666]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhang, Wei; Li, Yingxia |
| 作者单位 | 1.The National Center for Drug Screening, 189 Guoshoujing Road, Shanghai 201203, China 2.School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China; |
| 推荐引用方式 GB/T 7714 | Liu, Jian,Chen, Wuyan,Xu, Yechun,et al. Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors[J]. Bioorganic & medicinal chemistry,2015,23(9):1963-74. |
| APA | Liu, Jian,Chen, Wuyan,Xu, Yechun,Ren, Sumei,Zhang, Wei,&Li, Yingxia.(2015).Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors.Bioorganic & medicinal chemistry,23(9),1963-74. |
| MLA | Liu, Jian,et al."Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors".Bioorganic & medicinal chemistry 23.9(2015):1963-74. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。