Synthesis,Characterization And Biological Activity Of 1,3,4-thiadiazole Containing Pyrazolidinone/Hydroxy Pyrazole

Heterocyclic compounds have been playing a very significant role in the fields such as fine chemicals and organic synthesis.Especially,nitrogen-containing heterocycles occupy a vital position in the research and development of today's medicine and pesticide.Pyrazolidinone and hydroxyl pyrazole which have been widely used in medicine and other fields are an important class of pyrazole compounds and have a very good biological activity.As the activity center,the "nitrogen-carbon-sulfur" structure of 1,3,4-thiadiazole compounds can be the products for sterilization,desinsection,weeding,anti-cancer as well as viral and other effects-The reports on synthesis and the biological activity of containing a pyrazolidinone?hydroxyl pyrazole or 1,3,4-thiadiazole ring separately have been so many,but the report on containing both the two heterocyclic rings at the same time is very few.Therefore,design and synthesize which contains 1,3,4-thiadiazole structural unit pyrazolidinone/hydroxyl-pyrazole compounds and the study on compounds which contains the two structural units in the meantime is of great significance and application value.Based on our previous work and summarizd the relevant literature,2-hydrazino-5substituted-1,3,4-thiadiazole was respectively designed to raw materials the acrylamide,cinnamic acid ester derivatives and the sodium methoxide which were synthesized twenty-three unreported target compounds.The correctness structure of the synthesized compound determine by IR?NMR.According to solution crystallization method,cultured in ethanol to give the title compound and an organic single crystal V 7 and V 14 and X-ray diffraction of the resulting organic single crystal structure test.The results are consistent with IR and NMR analysis and determine further the structure of the synthesized target compounds.The novel of compound ? 2-chloro-5-(3-chloro-4-methoxyphenyl)-1,3,4-thiadiazole had been synthesized.The correctness structure of the synthesized compound determine by IR?NMR and the target compound V 14 organic single crystal structure analysis.Determination Act 96 at a certain concentration gradient,against Escherichia coli and Staphlococcus aureus of target compounds were synthesized antibacterial activity test.And the experimental results show that most of the target compounds had inhibitory activities.In the two bacteria showed some inhibitory activity against was better than the inhibitory activity against Escherichia coli,which is in the compound V 20 half inhibitory concentration of Escherichia coli IC50 reach 1.109mg/mL,half inhibitory concentration of Staphylococcus aureus IC50 reach 0.55mg/mL,in all of the compounds in the best inhibitory effect.