Synthesis Of1,3,4-Oxadiazole Compounds With Biological Activity

On account of their special molecular structure,1,3,4-oxadiazoles often show strongfluorescent properties and exhibit significant biological activities in anti-inflammatory,anticancer, antimicrobial, insecticidal, etc. Therefore, modified the1,3,4-oxadiazole moietywith other active functional groups by means of superposition principle of biological activity,more and more new compounds could have been synthesized.In this paper, some1,3,4-oxadiazoles with different biological effects were discussed asfollows.(1)A series of1,3,4-oxadiazoles with sulfide structure were synthesized, and theirantibacterial activity against Staphylococcus aureus, Escherichia coli and Bacillus subtiliswere studied. The results showed that compound modified with nitro group has a certaineffect on inhibition of the above bacteria.(2)Five kind of1,3,4-oxadiazoles modified with maleimide or chloroacetamide weredesigned and prepared, among which three compounds were involved in the phenomenon ofsignificant change of fluorescence intensity after with sulfhydryl compounds, which might bea new fluorescent probe for thiol dection.(3)A new kind of1,3,4-oxadiazole modified with coumarin and phosphate ester wassynthesized, and the enzymatic reaction on calf intestinal phosphatase (CIP) usingfluorescence analysis was preliminary investigated. The results showed that hydrolysis ofphosphate groups led to obvious changes in fluorescence intensity, and the incubation time,temperature and pH have a certain influence in the reaction system.In summary, several1,3,4-oxadiazole compounds in this thesis have shown certainbiological activities, which will provide some basic experimental data for further research anddevelopment.