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Synthesis and anti-HIV-1 activity evaluation of N-1-alkyl-5-halogeno-6-alkylamino uracils as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

Han Yan, Xiao-Wei Wang*, Ying Guo, Zhi-Li Zhang, Jun-Yi Liu*   

  1. 1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    2. State key Laboratory of Natural and Biomimetic Drug, Peking University Health Science Center, Beijing 100191 China
  • Received:2010-11-29 Revised:2011-02-10 Online:2011-03-15 Published:2011-03-15
  • Contact: Xiao-Wei Wang*, Jun-Yi Liu*

Abstract: N-1-alkyl-5-halogeno-6-alkylamino uracils, which are novel 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) analogues, were synthesized as the selective and potent non-nucleoside human immunodeficiency virus (HIV)-1 reverse transcriptase inhibitors. Some of the compounds showed potent inhibitory activity against HIV-1 reverse transcriptase. For instance, compounds 1d, 1m and 1n exhibited potent anti-HIV-1 activity with the IC50 values of 13.3, 11.7 and 3.15 µM, respectively, which are comparable to that of nevirapine (IC50 8.38 µM).

Key words: HIV-1 reverse transcriptase, Non-nucleoside reverse transcriptase inhibitors, HEPT analogues

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