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学科主题: 药学
题名:
The design and synthesis of N-1-alkylated-5-aminoaryalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors
作者: Lu, Xiao1; Chen, Yanli1; Guo, Ying1; Liu, Zhenming2; Shi, Yawei2; Xu, Yang1; Wang, Xiaowei1; Zhang, Zhili1; Liu, Junyi1,2
关键词: HIV-1 reverse transcriptase ; Non-nucleoside reverse ranscriptase inhibitors (NNRTIs) ; HEPT analogues
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2007-12-01
DOI: 10.1016/j.bmc.2007.07.058
卷: 15, 期:23, 页:7399-7407
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: REVERSE-TRANSCRIPTASE INHIBITORS ; HUMAN-IMMUNODEFICIENCY-VIRUS ; ANTIVIRAL ACTIVITY ; ANTI-HIV-1 AGENTS ; DERIVATIVES ; AIDS ; 1-&lt ; (2-HYDROXYETHOXY)METHYL&gt ; -6-(PHENYLTHIO)THYMINE ; THERAPY ; FUTURE ; NNRTIS
英文摘要:

Novel compounds 1a-u, which can be considered as hybrid analogues of MKC-442 and pyridinon, have been synthesized and evaluated as inhibitors of HIV-1 reverse transcriptase (HIV-1 RT). Starting from 6-methyuracil 2, 1-alkylated-5-bromomethyl-6-methyluracils 8 was prepared in four steps by hydroxylmethylation, etherification, N-1 alkylation, and bromination. Finally, compounds 1a-u were achieved in the displacement of 5-bromomethyl group by nucleophiles with amino compounds. Some of compounds 1a-u showed potent inhibitory activity against HIV-1 RT. The most active compounds showed activity in the low micromolecular range with IC50 values (IC50 0.82-5.09 mu M) comparable to that of nevirapine (IC50 10.60 mu M). The biological testing results are in accordance with the docking. (C) 2007 Elsevier Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000253489100019
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/57874
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, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100083, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drug, Beijing 100083, Peoples R China

Recommended Citation:
Lu, Xiao,Chen, Yanli,Guo, Ying,et al. The design and synthesis of N-1-alkylated-5-aminoaryalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2007,15(23):7399-7407.
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