Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives
文献类型：期刊论文
| 作者 | Cheng P[*]1; Chen JJ2; Huang N3; Wang RR3; Zheng YT3; Liang YZ1 |
| 刊名 | MOLECULES
 |
| 出版日期 | 2009 |
| 卷号 | 14期号:9页码:3176-3186 |
| 关键词 | (E)-N-phenylstyryl-N-alkylacetamides synthesis reverse transcriptase anti-HIV-1 activity |
| ISSN号 | 1420-3049 |
| 通讯作者 | picheng55@126.com |
| 合作状况 | 其它 |
| 英文摘要 | A series of (E)-N-phenylstyryl-N-alkylacetamides, 5, were synthesized by direct reduction-acetylation of beta-arylnitroolefins, followed by N-alkylation. The title compounds were characterized by (1)H-NMR, EIMS and IR analysis. All the synthesized compounds were assayed as HIV-1 non-nucleoside reverse transcriptase inhibitors. A SAR study revealed that when group R(1) in 5 was ortho-substituted, the resulting compounds showed better inhibitory activities against HIV-1 RT. Among the tested compounds, 5i (R(1) = 2-Br, R(2) = 3,5-difluorobenzyl) exhibited the highest enzyme activity, with a 88.89% inhibitory ratio against HIV-1 reverse transcriptase at the tested concentration. Further cell-based anti-HIV-1 assays showed that compound 5i exhibited a SI value of 29 with an EC(50) value of 4 mu M in C8166 cells. |
| 学科主题 | Chemistry, Organic |
| 收录类别 | SCI |
| 资助信息 | This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. |
| 原文出处 | 20091493176.pdf |
| 语种 | 英语 |
| 公开日期 | 2010-08-24 |
| 源URL | [http://159.226.149.42:8088/handle/152453/4659]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.School of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China 2.State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, the Chinese Academy of Sciences, Kunming 650204, China 3.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, the Chinese Academy of Sciences, Kunming 650223, China |
| 推荐引用方式 GB/T 7714 | Cheng P[*],Chen JJ,Huang N,et al. Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives[J]. MOLECULES,2009,14(9):3176-3186. |
| APA | Cheng P[*],Chen JJ,Huang N,Wang RR,Zheng YT,&Liang YZ.(2009).Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives.MOLECULES,14(9),3176-3186. |
| MLA | Cheng P[*],et al."Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives".MOLECULES 14.9(2009):3176-3186. |
入库方式： OAI收割
来源：昆明动物研究所
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