The Research Of Synthesis And Antibacterial Activity Of Nitrogen-containg Aryl Thiosemicarbazone

Nitrogen mustard compounds with high anti-tumor activity, were the first developed andused in clinical anticancer drugs, but there is treatment of low efficiency and poor selectivity,toxic side effects and other shortcomings; Polysubstituted pyrrole compounds andthiosemicarbazone compounds are found in recent years, with anti-bacterial, anti-fungal,anti-virus, anti-tumor, anti-parasitic and other biologically active substances. To get newantitumor drugs which have lower side effects and higher therapeutic index, this researchparallel to nitrogen mustard derivatives and pyrrole derivatives were introduced into theN4-substituted thiosemicarbazide, thus synthesized 12 nitrogen mustard class ofthiosemicarbazone and 18 pyrrole thiosemicarbazone, hoping that they have better biologicalactivity and lower side effects .The contents are as follows :1 Summarized synthesis, application and recent progress of nitrogen mustards , pyrrolederivatives and thiosemicarbazone .2 Prepared 12 derivatives of nitrogen mustards of thiosemicarbazone ; Studied therelationship between the solvent , the temperature, material ratio , the structures of targetcompounds and yields. Give the best reaction conditions ; The products were identified by IR,1H NMR and MS .3 Prepared 3 pyrrole derivatives by Paal-Knorr pyrrole with microwave irradiationmethod . To replace the pyrrole and semicarbazide synthesized 18 compounds pyrrolicthiosemicarbazone . Studied the relationship between the solvent , the temperature, materialratio , the structures of target compounds and yields. Give the best reaction conditions ; Theproducts were identified by IR, 1H NMR and MS.4 By slip diffusion method to sulfa antimicrobial agents sulfamethazine,sulfa-methoxy-pyrimidine, sulfamonomethoxine and quinolones such as norfloxacinantithesis to Escherichia coli and Staphylococcus aureus was the test model, the 30synthesized compounds were tested antibacterial activity screening. The results show that thesynthesized compounds against Escherichia coli and Staphylococcus aureus had strong antibacterial activity, antibacterial activity of many compounds is stronger than the controldrugs.