Synthesis And DNA Cleavage Activity Of Novel Pyrazole Derivatives

Pyrazole and pyrazole derivatives occupied an important position in pesticide and medicinal chemistry because of a wide range of pharmaceutical activities. As pesticides, pyrazole derivatives show highly fungicide, insecticides, antifungal activity, herbicidal activity. As medicines, a lot of pyrazole and pyrazole derivative show antimicrobial activity, antitumor activity, anticancer, cytotoxic activity, hypoglycemic activity, antiviral activity and many other biological activities, In recent years, there has been an enormous increase of interest among the chemists on the research of the pyrazole derivatives.In this thesis, benzylamine and ethyl bromoacetate were used as the starting materials, based on the methods of nucleophilic substitution, nucleophilic addition, Claisen condensation, and then reacted with hydrazine. At last,17target compounds and4relatde intermediates were obtained, and all of the target compounds have never been reported in the literatures. All the target compounds were characterized by IR、1H NMR、13C NMR, among the target compounds, two compounds were characterized by X-Ray single crystal diffraction measurement. The constitutional formula of target compounds as follows:In addition, the interaction of plasmid pUC19DNA with ligands in the presence of Cu(II) complexes respectively was monitored by Agarose gel electrophoresis. Then we investigate the reaction conditions of different metal complexes, different pH, concentration and reaction time on the experiment, and at last we choose the best reaction condition of the reaction. The experimental results show that:the cleavage activity of pUC19DNA is well when the nitrogen atom unsubstituent of the pyrazole ring and if the compound contained the fluorine or chlorine, the result is not as well as the4e1, we need to investigate the reason through the experiments. At last, we approved the reaction mechanism is Hydrolysis mechanism.