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
ISSN1420-3049
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
资助信息Dr Pi Cheng in Centre South University
学科领域Chemistry, Organic
DOI10.3390/molecules14093176
收录类别SCI
语种英语
WOS研究方向Chemistry
WOS类目Chemistry, Organic
WOS记录号WOS:000270201900006
引用统计
被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
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.
条目包含的文件
文件名称/大小 文献类型 版本类型 开放类型 使用许可
201202230046.pdf(250KB) 开放获取--请求全文
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Cheng, Pi]的文章
[Chen, Ji-Jun]的文章
[Huang, Ning]的文章
百度学术
百度学术中相似的文章
[Cheng, Pi]的文章
[Chen, Ji-Jun]的文章
[Huang, Ning]的文章
必应学术
必应学术中相似的文章
[Cheng, Pi]的文章
[Chen, Ji-Jun]的文章
[Huang, Ning]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

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。