Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives
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摘要: 目的 设计合成吡啶-2-酮酰胺类新型化合物并对其进行抗病毒活性研究。 方法 以药效团模型为指导,经Heck反应、选择性硝化反应、催化氢化反应、酰化反应以及开环重排反应等设计合成目标化合物。所合成化合物经1H NMR谱图进行确证,并对其进行抗HBV-DNA复制活性筛选。 结果 设计合成的新型-2-吡啶酮酰胺类化合物对HBV-DNA复制都有一定的抑制活性,其中化合物6h、6e和6a抑制活性最好,值得进一步关注。 结论 吡啶环N原子上接有对乙氧基苯基时抑制HBV-DNA活性最好,为活性必须基团。
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关键词:
- 2-吡啶酮酰胺类化合物 /
- 化学合成 /
- 抗乙肝病毒活性
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.-
Key words:
- 2-pyridyl ketone amide /
- chemical synthesis /
- anti-HBV activity
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