| Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives | |
| Cheng P*1; Chen JJ2; Huang N3; Wang RR3; Zheng YT3; Liang YZ1; picheng55@126.com | |
| 2009 | |
| 发表期刊 | MOLECULES
 |
| ISSN | 1420-3049 |
| 卷号 | 14期号:9页码:3176-3186 |
| 合作性质 | 其它 |
| 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. |
| 关键词 | (e)-n-phenylstyryl-n-alkylacetamides Synthesis Reverse Transcriptase Anti-hiv-1 Activity |
| 学科领域 | Chemistry, Organic |
| 资助者 | This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. ; This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. ; This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. ; This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. |
| URL | 查看原文 |
| 收录类别 | SCI |
| 语种 | 英语 |
| 资助者 | This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. ; This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. ; This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. ; This work was partly supported by young teachers' scientific researching foundation for Dr Pi Cheng in Centre South University. |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/4659 |
| 专题 | 科研部门_分子免疫药理学（郑永唐） 科研部门_动物模型与人类重大疾病机理重点实验室 |
| 通讯作者 | picheng55@126.com |
| 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.,...&picheng55@126.com.(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. |
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| 文件名称/大小 | 文献类型 | 版本类型 | 开放类型 | 使用许可 | ||
| 20091493176.pdf（250KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | 请求全文 | |
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