Synthesis And Biological Evaluation Of ?-alkamine Derivatives As Novel Neuraminidase Inhibitors

Influenza is a common respiratory disease caused by influenza virus,which is one of the major killers that affect the healthy life of human beings.Neuraminidase inhibitors?NIs?as anti-influenza virus drugs is most effective.It can selectively inhibit neuraminidase?Neuraminidase,NA?,and prevent Progeny virus from replication and release in host cells.At present,because of the anti-genic variability of influenza virus,the drug resistance of NIs has been increasing year by year,so the research and development of new NIs has been imminent.This research work is divided into three parts:firstly,the epigoitrin was used as the lead compound,through structure modification and optimization.Synthesis target compounds through aldehyde addition,cyano reduction,acylation and alkylation of N-acylation,N-alkylation,N-guanidination with the commercialization of aromatic aldehydes as the starting material.The compounds were characterized by ¹H NMR,¹³C NMR,IR,HRMS and other methods;Secondly,using fluorescent substrate detection principle to determinate of these compounds'NA inhibitory activity,and calculate IC₅₀ value;Thirdly,explanation the relationship between the NA inhibitory activity of the compounds and theirs chemical structure by the mechanism of receptor protein and ligand small molecule.