| 新型吡啶-2-酮酰胺类化合物的设计、合成及抗乙肝病毒活性研究 |
| 投稿时间：2012-04-06 修订日期：2012-07-07 点此下载全文 |
| 引用本文：张明峰,吕志良,李科.新型吡啶-2-酮酰胺类化合物的设计、合成及抗乙肝病毒活性研究[J].药学实践杂志,2013,31(2):102~107 |
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| 基金项目:国家自然基金(21172259);全军特殊环境药物研究重点实验室资助项目 |
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| 中文摘要: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。 |
| 中文关键词:2-吡啶酮酰胺类化合物 化学合成 抗乙肝病毒活性 |
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| Design, synthesis and anti-HBV activity of novel 2-prindyl ketone derivatives |
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| 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. |
| keywords:2-pyridyl ketone amide chemical synthesis anti-HBV activity |
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