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The design and synthesis of N-1-alkylated-5-aminoaryalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors
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
2007-12-01
DOI10.1016/j.bmc.2007.07.058
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
引用统计
被引频次:32[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/400002259/57874
专题北京大学药学院_化学生物学系
北京大学药学院
北京大学药学院_药物化学系
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
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GB/T 7714
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.
APA Lu, Xiao.,Chen, Yanli.,Guo, Ying.,Liu, Zhenming.,Shi, Yawei.,...&Liu, Junyi.(2007).The design and synthesis of N-1-alkylated-5-aminoaryalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,15(23),7399-7407.
MLA Lu, Xiao,et al."The design and synthesis of N-1-alkylated-5-aminoaryalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 15.23(2007):7399-7407.
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