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Volume 31 Issue 2
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2013  >  31(2): 102-107

ZHANG Ming-Feng, LV Zhi-liang, LI Ke. Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 102-107. doi: 10.3969/j.issn.1006-0111.2013.02.006
Citation: ZHANG Ming-Feng, LV Zhi-liang, LI Ke. Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 102-107. doi: 10.3969/j.issn.1006-0111.2013.02.006
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Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives

doi: 10.3969/j.issn.1006-0111.2013.02.006

  • Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • Received Date: 2012-04-06
  • Rev Recd Date: 2012-07-07
  • Objective To design and synthesize the new 2-pyridyl ketone amide derivatives and test the antiviral activity. Methods According to the pharmacophore model, a new class of 2-pyridyl ketone amide derivatives was designed, which were synthesized by Heck reaction, selective nitration reaction, catalytic hydrogenation reaction, acylation reaction and the open-loop rearrangement reaction. All the synthesized compounds were confirmed by 1H NMR, and their anti-HBV-DNA replication activity were determined. Results The designed novel 2-pyridyl ketone amide derivatives had inhibitory activity against HBV-DNA replication. Among them, compounds 6h、6e and 6a showed the best inhibitory activity. Conclusion When the 4-ethoxyl phenyl group was attached on the N atom of the benzyl ring, the compounds revealed good inhibitory activity.
  • [1] Lavanchy D. Hepatitis B virus epidemiology, disease burden, treatment, and current and emerging prevention and control measures[J]. J Viral Hepatiti, 2004, 11 (2), 97.
    [2] http://www.who.int/mediacentre/factsheets/fs204/en/.
    [3] Dienstag JL. Hepatitis B Virus Infection[J]. New Eng J Med, 2008, 359 (14), 1486.
    [4] Lui YYN,Chan HLY. Treatment of chronic hepatitis B:focus on telbivudine[J]. Expert Rev Anti Infect Ther, 2009, 7 (3), 259.
    [5] Cheng PN,Chang TT. Entecavir:a potent antiviral with minimal long-term resistance in nucleoside-naive chronic hepatitis B patients[J]. Expert Rev Anti Infect Ther, 2008, 6 (5), 569.
    [6] Lv Z,Sheng C,Wang T,et al. Design, synthesis, and antihepatitis B virus activities of novel 2-pyridone derivatives[J]. J Med Chem, 2009, 53, 660.
    [7] Dong H,Li K,Zheng C,et al. Synthesis and antitumor activity of novel 3-(substituted amino)-chromone derivatives[J]. Acta Chim Sin, 2009, 67(8), 819.
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Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives

doi: 10.3969/j.issn.1006-0111.2013.02.006
  • Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • Received Date: 2012-04-06
  • Rev Recd Date: 2012-07-07

Abstract: Objective To design and synthesize the new 2-pyridyl ketone amide derivatives and test the antiviral activity. Methods According to the pharmacophore model, a new class of 2-pyridyl ketone amide derivatives was designed, which were synthesized by Heck reaction, selective nitration reaction, catalytic hydrogenation reaction, acylation reaction and the open-loop rearrangement reaction. All the synthesized compounds were confirmed by 1H NMR, and their anti-HBV-DNA replication activity were determined. Results The designed novel 2-pyridyl ketone amide derivatives had inhibitory activity against HBV-DNA replication. Among them, compounds 6h、6e and 6a showed the best inhibitory activity. Conclusion When the 4-ethoxyl phenyl group was attached on the N atom of the benzyl ring, the compounds revealed good inhibitory activity.

ZHANG Ming-Feng, LV Zhi-liang, LI Ke. Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 102-107. doi: 10.3969/j.issn.1006-0111.2013.02.006
Citation: ZHANG Ming-Feng, LV Zhi-liang, LI Ke. Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(2): 102-107. doi: 10.3969/j.issn.1006-0111.2013.02.006
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