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Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. - synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues 期刊论文

编号：

c4c0cf43-c9b2-4e58-ba6c-a0c378060829
作者：

Ji, Lei; Chen, FenEr; Feng, XiaoQing; De Clercq, Erik; Balzarini, Jan; Pannecouque, Christophe
语种：

English
期刊：

CHEMICAL & PHARMACEUTICAL BULLETIN ISSN：0009-2363 2006 年 54 卷 9 期 (1248 - 1253) ; SEP
收录：
关键词：

HIV-1 reverse transcriptase inhibitor antiviral activity synthesis 3D-QSAR 6-(1-naphthoyl)
摘要：

A series of novel 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) analogues bearing a 6-(1-naphthoyl) group of non-nucleoside human immunodeficiency virus (HIV) reverse transcriptase inhibitors were synthesized and evaluated for their activity against HIV-1 and HIV-2. It was found that most of these compounds showed good activity against HIV-1. Among them, compound 5-isopropyl-6-(1-naphthoyl)-1-[(2E)-3-phenylallyl]-2,4-pyrimidinedione (23) displayed the greatest inhibitory potency (IC50=0.14 mu m), which is about 35-fold more active than HEPT and DDI. To rationalize the relationships between structure and activity of these novel compounds, a three-dimensional quantitative structure-activity relationship (3D-QSAR) model was also generated. The results provided a tool for guiding the further design of more potent antiviral agents and for predicting the affinity of related compounds.
推荐引用方式
GB/T 7714：

Ji Lei,Chen Fen-Er,Feng Xiao-Qing, et al. Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. - synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues [J].CHEMICAL & PHARMACEUTICAL BULLETIN,2006,54(9):1248-1253.
APA：

Ji Lei,Chen Fen-Er,Feng Xiao-Qing,De Clercq Erik,&Pannecouque Christophe.(2006).Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. - synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues .CHEMICAL & PHARMACEUTICAL BULLETIN,54(9):1248-1253.
MLA：

Ji Lei, et al. "Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. - synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues" .CHEMICAL & PHARMACEUTICAL BULLETIN 54,9(2006):1248-1253.

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