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Synthesis of 1-(alkyl)-5-dimethylamino-6-phenethyluracils as potent nonnucleoside HIV-1 RT inhibitors
Wang, Xiaowei; Chen, Yanli; Guo, Ying; Li, Amin; Ma, Xiaoyan; Liu, Junyi
关键词5-dimethylamino 6-phenethyluracils HIV-1 reverse transcriptase nonnucleoside reverse transcriptase inhibitors
刊名SYNTHETIC COMMUNICATIONS
2007
DOI10.1080/00397910701412737
37期:14页:2421-2431
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]1-&lt ; (2-HYDROXYETHOXY)METHYL&gt ; -6-(PHENYLTHIO)THYMINE HEPT ; ACYCLOURIDINE DERIVATIVES ; REVERSE-TRANSCRIPTASE ; ANTI-HIV-1 AGENTS ; ANALOGS ; SERIES
英文摘要

1-(Alkyl)-5-dimethylamino-6-phenethyl uracils (1) and (2) are analogs of MKC-442, which is a very potent inhibitor of HIV-1 reverse transcriptase. The target compound 1 was synthesized by the first approach, from the corresponding 1,3-dibenzyl-5-(dimethylamino)-6-phenethylpyrimidine-2,4(1H,3H)-dione (7), which was synthesized in four steps from 6-methyluracil (3) by nitration, benzylation, reduction, and methylation of the amino group. Compound 7 was then debenzylated to give the complete deprotected compound 8 with very low yield. To improve the yield, another pathway was developed for introducing the ethoxymethyl group at N-1 of the uracil ring first. The result of adjusting reaction sequences increased the overall yield dramatically. All synthesized compounds were tested for their inhibition of HIV-1 reverse transcriptase, and moderate activity was found for target compound 1.

语种英语
WOS记录号WOS:000248145900015
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.bjmu.edu.cn/handle/400002259/62167
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, Dept Biol Chem, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Wang, Xiaowei,Chen, Yanli,Guo, Ying,et al. Synthesis of 1-(alkyl)-5-dimethylamino-6-phenethyluracils as potent nonnucleoside HIV-1 RT inhibitors[J]. SYNTHETIC COMMUNICATIONS,2007,37(14):2421-2431.
APA Wang, Xiaowei,Chen, Yanli,Guo, Ying,Li, Amin,Ma, Xiaoyan,&Liu, Junyi.(2007).Synthesis of 1-(alkyl)-5-dimethylamino-6-phenethyluracils as potent nonnucleoside HIV-1 RT inhibitors.SYNTHETIC COMMUNICATIONS,37(14),2421-2431.
MLA Wang, Xiaowei,et al."Synthesis of 1-(alkyl)-5-dimethylamino-6-phenethyluracils as potent nonnucleoside HIV-1 RT inhibitors".SYNTHETIC COMMUNICATIONS 37.14(2007):2421-2431.
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