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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. 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*

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

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