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Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue  期刊论文  

  • 编号:
    4f816828-a941-4c5a-9eb1-3583f274c73f
  • 作者:
    Wan, ZhengYong[1] Yao, Jin[1] Mao, TianQi[1,2] Wang, XinLong[1] Wang, HaiFeng[1] Chen, WenXue[1] Yin, Hong[1] Chen, FenEr[1,2] De Clercq, Erik[3] Daelemans, Dirk[3] Pannecouque, Christophe[3]
  • 语种:
    English
  • 期刊:
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY ISSN:0223-5234 2015 年 102 卷 (215 - 222) ; SEP 18
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  • 摘要:

    Based on molecular simulation, the etravirine-VRX-480773 hybrids previously disclosed by our group were optimized to yield novel pyrimidine sulfonylacetanilides 8 with improved activity against a panel of seven clinically relevant single and double mutant strains of HIV-1. The improvement in potency in this in vitro model of HIV RNA replication partly validates the mechanism by which this class of allosteric pyrimidine derivatives inhibits the reverse transcriptase (RT), and represents a remarkable step forward in the development of anti-HIV drugs. (C) 2015 Elsevier Masson SAS. All rights reserved.

  • 推荐引用方式
    GB/T 7714:
    Wan Zheng-Yong,Yao Jin,Mao Tian-Qi, et al. Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue [J].EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2015,102:215-222.
  • APA:
    Wan Zheng-Yong,Yao Jin,Mao Tian-Qi,Wang Xin-Long,&Pannecouque Christophe.(2015).Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue .EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,102:215-222.
  • MLA:
    Wan Zheng-Yong, et al. "Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue" .EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 102(2015):215-222.
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