Synthesis of Acyclovir–Nortriptyline Conjugates with Amino Acid Ester as Anti-enteroviral Agents

• Main Authors: Huei-ran Syu, 許惠然
• Other Authors: 胡紀如
• Format: Others
• Language: zh-TW
• Published: 2014
• Online Access: http://ndltd.ncl.edu.tw/handle/79vkum

碩士 === 國立中央大學 === 化學學系 === 102 === Virus-related infections pose a serious global threat to human health, causing many human diseases and deaths. Particularly, treatment of RNA viruses lacks effective drugs and vaccines, largely because such viruses mutate rapidly. The laboratory of Professor Jih Ru Hwu are participating in the European Union’s Seventh Framework Programme. Out project is called, “Small-molecule Inhibitor Leads versus Emerging and Neglected RNA viruses’’ , and focuses on discovering drugs for treating Flaviviridae, Picronviridae, Paramyxoviridae, Alphaviridae, Arenaviridae, Bunyaviridae, Coronaviridae, Noroviridae,and Rhabdoviridae. Our laboratory has combined two antiviral activity-related drugs together. Experimental results indicate that acyclovir–nortriptyline conjugates inhibit enterovirus replication activity. Correspondingly, this study uses a similar architecture design to molecular structure. This study focuses on acyclovir–nortriptyline conjugates with amino acid esters as the target products. The synthetic method uses coupling reagent N,N’- dicyclohexylcarbodiimide and catalyst 4-(dimethylamino)pyridine react with amino acids, such that the functional group from the amine to better leaving group, and then react with acyclovir derivatives. Finally, a protecting group is removed by piperidine to achieve the final target. The target structures are confirmed by nuclear magnetic resonance spectrometry and high resolution mass spectrometers.