| Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives | |
Cheng, Pi1; Chen, Ji-Jun2 ; Huang, Ning3; Wang, Rui-Rui3; Zheng, Yong-Tang3; Liang, Yi-Zeng1
| |
| 2009-09-01 | |
| 发表期刊 | MOLECULES
 |
| ISSN | 1420-3049 |
| 卷号 | 14期号:9页码:3176-3186 |
| 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 |
| DOI | 10.3390/molecules14093176 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000270201900006 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/4776 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 作者单位 | 1.Cent S Univ, Sch Chem & Chem Engn, Changsha 410083, Peoples R China 2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China 3.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Lab Mol Immunopharmacol, Kunming 650223, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cheng, Pi,Chen, Ji-Jun,Huang, Ning,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, Pi,Chen, Ji-Jun,Huang, Ning,Wang, Rui-Rui,Zheng, Yong-Tang,&Liang, Yi-Zeng.(2009).Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives.MOLECULES,14(9),3176-3186. |
| MLA | Cheng, Pi,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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