Synthesis And Biological Evaluation Of 1,3-oxazole-2-thione-based Neuraminidase Inhibitors

Since twenty-first century, the enhancement of the variability of influenza viruses and the frequent outbreak of highly pathogenic avian influenza in the world have seriously affected the daily life and economic development of human beings. At present, vaccination and drug treatment are the main measures to prevent and control influenza. However, the characteristics of influenza virus subtypes are very easy to mutate, which makes people can not accurately predict the outbreak of influenza virus, thus, conventional influenza vaccines can't do anything about the new flu virus. Therefore, exploring new safe and effective anti influenza virus drugs has become a hot research topic.Neuraminidase (NA) inhibitor is a new class of anti-influenza virus drugs developed in recent years,it has a good effect for the treatment and prevention of influenza. Among them,Isatis indigotica Fort and the existing preparations have good antiviral activity, the research shows that epigoitrin is one of the main effective components of Radix Isatidis to against influenza virus. Therefore, in this thesis epigoitrin was used as the leading compound, through the modification of its structure, the highly active neuraminidase inhibitors were obtained.The main research work of this thesis are: take aldehydes as starting material,1,3-oxazole-2-thione-based neuraminidase inhibitors were synthesized through aldehyde addition, cyano reduction,hydroxy amino condensation and N-substitution. After that,we obtained the inhibition ratio and IC50 value of 1,3-oxazole-2-thione neuraminidase inhibitors through Microplate Reader. Finally, the high bioactivity of 1,3-oxazole-2-thione-based neuraminidase inhibitors were analyzed and explained by molecular docking.