| dc.description.abstract | Virus-related diseases pose a serious global treat to human health. In particular, RNA viruses lack effective drugs and vaccines, largely owing to the rapid mutation rate of such viruses. Therefore, the Seventh Framework Programme in the European Union has approved a project that focuses on drugs discovery towards Flaviviridae and Picornaviridae. Our laboratory participating in this program, referred to as SILVER, Our laboratory is devoting its efforts developing lead candidate.
The laboratory of Professor Jih Ru Hwu has combined two antiviral activity-related drugs together. Based on those results, nortriptyline–acyclovir conjugates to inhibit of enterovirus replication activity, Correspondingly, this study use a similar architecture design to molecular structure. Our indicate that benzhydryl or benzhydrylidene is similar to nortriptyline, so we replaces ＂nortriptyline＂ with benzhydryl or benzhydrylidene. This study focuses on benzhydryl–acyclovir and benzhydrylidene–acyclovir conjugates as the target product, The synthetic method uses triphosgene react with amines, allowing for functional group from amine to isocyanate, and then reacting with acyclovir derivatives.
The target structures are confirmed by nuclear magnetic resonance, high resolution mass spectrometers, and infrared spectroscopy. Finally, a protecting group is removed to achieve the final target. For the conjugated compound 21 which inhibits ＂EV71＂ activity, its EC50 = 23.7 μM. | en_US |