Synthesis of Nucleoside–Amantadine Carbamides as Antiviral Agents
| Autor: | Shin-Hong Liu, 劉信宏 |
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| Rok vydání: | 2013 |
| Druh dokumentu: | 學位論文 ; thesis |
| Popis: | 101 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. |
| Databáze: | Networked Digital Library of Theses & Dissertations |
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