Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives

doi:10.3390/molecules14093176

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	Synthesis and Anti-Human Immunodeficiency Virus Type 1 Activity of (E)-N-Phenylstyryl-N-alkylacetamide Derivatives
	Cheng, Pi 1; Chen, Ji-Jun2 ; Huang, Ning 3; Wang, Rui-Rui 3; Zheng, Yong-Tang 3; Liang, Yi-Zeng 1
刊名	MOLECULES
	2009-09-01
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
DOI	10.3390/molecules14093176
文献子类	Article
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
WOS关键词	REVERSE-TRANSCRIPTASE INHIBITORS ; BIOLOGICAL EVALUATION ; IN-VITRO ; HIV-1 RT ; RNASE-H ; INTEGRASE ; DESIGN
WOS研究方向	Chemistry
语种	英语
WOS记录号	WOS:000270201900006
资助机构	Dr Pi Cheng in Centre South University
公开日期	2012-03-21
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn:8080/handle/151853/4776]
专题	昆明植物研究所_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.