The Synthesis Of Benzofurans And The Inhibitory Activity To Monoamine Oxidase

In recent years,the structure and catalytic mechanism of monoamine oxidase has been illustrated.The study of monoamine oxidase inhibitor has attracted many attentions.Three aspects are involved in this thesis as follows:First,small molecule selenium bromine as raw materials,the biological activity benzofuran compounds containing selenium was synthesized with a variety of substituted o-allyl phenols by electrophilic cyclizationreaction.Synthesis of a series of derivatives containing biological activity triazole ring,isoxazole ring by propargyl,1,3 dipolar cycloaddition reaction.Second,brominated polystyrene resin selenium load carrier,the resin immobilization by electrophilic cyclizationreaction,and then by multi-step solid state reaction,oxidative cleavage reaction successfully synthesized benzofuran compounds containing triazole ring,isoxazole ring.Last,the benzofuran compounds inhibitory activity to monoamine oxidase were detected by fluorescent probe.The results show that among all the benzofuran compounds,10f whose IC50 is 110.05 μM shows the best inhibitory activity against MAO-B,and 3e only shows the inhibitory activity against MAO-A,while 3g、10a、10b、10d show the better inhibitory activity against MAO-B.