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学科主题: 药学
题名:
Synthesis of 1-(alkyl)-5-dimethylamino-6-phenethyluracils as potent nonnucleoside HIV-1 RT inhibitors
作者: 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
发表日期: 2007
DOI: 10.1080/00397910701412737
卷: 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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62167
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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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

Recommended Citation:
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.
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