合成「核?」與「金剛胺」連結之?鍵化合物作為抗病毒藥劑; Synthesis of Nucleoside–Amantadine Carbamides as Antiviral Agents

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题名:	合成「核?」與「金剛胺」連結之?鍵化合物作為抗病毒藥劑;Synthesis of Nucleoside–Amantadine Carbamides as Antiviral Agents
作者:	劉信宏;Liu,Shin-Hong
贡献者:	化學學系
关键词:	抗病毒藥劑;核?;金剛胺;antiviral agents;nucleoside;amantadine
日期:	2013-07-25
上传时间:	2013-08-22 11:39:39 (UTC+8)
出版者:	國立中央大學
摘要:	病毒所造成的危害是人類面臨的重大問題，其中又以RNA病毒具有較高的變異性，至今仍缺乏合適的藥物和疫苗。「歐盟第七架構計畫」中更將「黃病毒科」、「微小核醣核酸病毒科」和「副黏液病毒科」列為優先針對目標，並對其對應藥物進行合成和優化。本實驗室參與了這項定名為SILVER之計畫，致力於新藥的開發。由於「金剛胺」是最早用於抑制流感病毒的抗病毒藥，該藥對成年患者的療效及安全性已得到廣泛認同，且本實驗室以「核?」鍵結「香豆素」，發現其對於「C型肝炎病毒」具有良好的抑制活性，所以我們採用類似的架構設計新分子，將「金剛胺」與各種核?衍生物以?鍵結合為目標。其合成方法先將「金剛胺」藉由「三光氣」從胺基反應成「異氰酸酯」，再與矽保護的核?衍生物進行加成反應，並利用核磁共振光譜儀和高解析質譜儀鑑定結構，證實我們成功地合成目標分子。此外我們將「腺?」與「阿糖胞?」對於「金剛烷異氰酸酯」反應時的反應性不同，以及使用FT–IR圖譜判定目標產物的反應位置進行探討。最後我們也對目標產物進行水溶、脂溶與活性的測定，探討是否具有開發成抗病毒藥物的潛力。 Many human diseases and deaths are caused by viruses. RNA viruses generally have very high mutation rates, there are lack of suitable drugs and vaccines to control them. To solve these problems, Seventh Framework Programme in European Union has proved a project that focus on drugs discovery towards dengue-, entero- and paramyxoviruses. Our laboratory participating in this program, referred to as SILVER. Our laboratory is devoting its efforts developing relates drug. Since amantadine is the first antiviral drug for inhibits the influenza virus. Its efficacy and safety for adult patients has been extensively recognized. A series of nucleoside–coumarin conjugates with potent activity toward HCV were synthesized at our laboratory. The developed molecules herein were designed with a similar architecture. The goal of study was to use amantadine and a variety of nucleoside derivatives with carbamide. The synthesis involved reacting amantadine with triphosgene, allowing the functional group transfer from amine to isocyanate, then reacting with nucleoside analogous by addition reaction. The target structures were examined by nuclear magnetic resonance and high-resolution mass spectrometry. The reactivities of reactants adenosine and cytarabine with 1-adamantyl isocyanate were discussed. FT–IR spectra were used to determine the reaction position of the target product. Finally, the solubility in water, the solubility in lipid, and the activity are determined.
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