| 新型二氢吡啶类化合物的合成及其抗乙型肝炎病毒活性研究 |
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| 引用本文： | 郭真,王晓奎,章天,徐晓倩,郑志兵,钟武,赵国明,李松. 新型二氢吡啶类化合物的合成及其抗乙型肝炎病毒活性研究[J]. 解放军药学学报, 2009, 25(6): 471-475 |
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| 作者姓名： | 郭真 王晓奎 章天 徐晓倩 郑志兵 钟武 赵国明 李松 |
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| 作者单位： | 军事医学科学院毒物药物研究所,北京,100850;江西中医学院,江西,南昌,330006;中国医学科学院医药生物技术研究所,北京,100050;沈阳药科大学,辽宁,沈阳,110016 |
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| 基金项目： | 国家高技术研究发展计划(863计划)，国家重大科技专项-重大新药创制 |
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| 摘 要： | 目的合成全新的二氢吡啶类化合物,并对其抗乙型肝炎病毒（HBV）复制活性进行研究,以获得新型的抗病毒药物先导物。方法以芳杂环取代的二氢嘧啶类化合物为模板,通过比较分子场分析,设计全新的二氢吡啶类化合物。以乙酰乙酸乙酯,芳香酸为起始原料,分别经胺化、烷基化反应,再与芳香醛缩合关环得到最终目标化合物,并对其体外抑制HBV的活性进行试验。结果合成了未见文献报道的全新二氢吡啶类化合物13个,经1HNMR和MS确定了结构,部分化合物显示了对HBV DNA复制的抑制作用。化合物6f表现出较强的抑制病毒复制活性,体外活性优于阳性对照药拉米夫定。结论二氢吡啶类化合物做为一类全新结构的抗HBV化合物,值得进行深入研究。
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| 关 键 词： | 乙型肝炎病毒 二氢吡啶 比较分子场分析 病毒衣壳 |
Design and Synthesis of Novel Dihydropyridine Analogs as Anti-HBV Compounds1 |
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| GUO Zhen,WANG Xiao-Kui,ZHANG Tian,XU Xiao-Qian,ZHENG Zhi-Bing,ZHONG Wu,ZHAO Guo-Ming,LI Song. Design and Synthesis of Novel Dihydropyridine Analogs as Anti-HBV Compounds1[J]. Pharmaceutical Journal of Chinese People's Liberation Army, 2009, 25(6): 471-475 |
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| Authors: | GUO Zhen WANG Xiao-Kui ZHANG Tian XU Xiao-Qian ZHENG Zhi-Bing ZHONG Wu ZHAO Guo-Ming LI Song |
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| Affiliation: | (Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Beijing 100850 China;Jiangxi University of Traditional Chinese Medicine,Nanchang 330006,Jiangxi China;Institute of Medicinal and Biotecnology,Chinese Academy of Medical Sciences ＆ Peking Union Medical College,Beijing 100050 China;Shenyang Pharmaceutical University,Shenyang 110016,Liaoning China) |
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| Abstract: | Aim To synthesize novel dihydropyridine analogs as anti-HBV drug candidates.Methods Based on heteroaryldihydropyrimidines(HAPs) which was discovered as highly potent non-nucleosidic inhibitors of HBV replication in vitro and in vivo,the novel dihydropyridine analogs were designed by comparative molecular field analysis methods.The starting materials,ethyl acetoacetate and aromatic acid,were aminated and C-alkylated respectively and then cyclocondensed with proper aromatic aldehyde to yield the designed dihy... |
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| Keywords: | hepatitis B virus dihydropyridine comparative molecular field analysis capsid |
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