1-芳基-5-碘-6-苄基尿嘧啶的合成及作为非核苷类HIV-1 RT抑制剂的活性评估

1-芳基-5-碘-6-苄基尿嘧啶的合成及作为非核苷类HIV-1 RT抑制剂的活性评估

王惟, 李立, 刘畅, 张亮, 闫寒, 张志丽, 王孝伟, 刘俊义^*

1. 北京大学医学部天然药物及仿生药物国家重点实验室; 药学院化学生物学系, 北京 100191
2. 首都医科大学化学生物学与药学院, 北京 100069

收稿日期:2010-04-16 修回日期:2010-06-10 出版日期:2010-07-15 发布日期:2010-07-15
通讯作者: 刘俊义*

Synthesis and biological evaluation of novel 1-aryl-5-iodo-6-benzyluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors

Wei Wang, Li Li, Chang Liu, Liang Zhang, Han Yan, Zhi-Li Zhang, Xiao-Wei Wang, Jun-Yi Liu^*

1. State Key Laboratory of Natural and Biomimetic Drugs; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
2. School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China

Received:2010-04-16 Revised:2010-06-10 Online:2010-07-15 Published:2010-07-15
Contact: Jun-Yi Liu*

摘要/Abstract

摘要：

已报道的化合物6-苄基-1-苄基甲基-5-碘尿嘧啶,有很强的抗HIV-1的活性。合成此化合物的类似物,得到1a-1i 9个新化合物, 并进行了活性检测, 新化合物活性较弱。

关键词: HIV-1逆转录酶, 非核苷类抑制剂, HEPT类似物

Abstract: We have synthesized the novel compounds 1a-1i, which are a series of hybrid analogues to 6-benzyl-1-(benzyloxymethyl)-5-iodouracil, a compound showing strong activity against HIV-1. We also evaluated the activity of these compounds as the inhibitors of HIV-1 reverse transcriptase (HIV-1 RT), and they have demonstrated moderate activity.

Key words: HIV-1 reverse transcriptase, Non-nucleoside reverse transcriptase inhibitors, 1-[(2-Hydroxyethoxy)methyl]-6-phenylthiothymine

中图分类号:

R916

Supporting:

Foundation items: National Natural Science Foundation of China (Grant No. 20672008, and 20972011).
^*Corresponding author. Tel.: 86-10-82801706

王惟, 李立, 刘畅, 张亮, 闫寒, 张志丽, 王孝伟, 刘俊义^*. 1-芳基-5-碘-6-苄基尿嘧啶的合成及作为非核苷类HIV-1 RT抑制剂的活性评估[J]. .

Wei Wang, Li Li, Chang Liu, Liang Zhang, Han Yan, Zhi-Li Zhang, Xiao-Wei Wang, Jun-Yi Liu^*. Synthesis and biological evaluation of novel 1-aryl-5-iodo-6-benzyluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors [J]. .

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