Preparation Of Acylthiourea And Carbamate And Their Inhibitory Activity Towards Epoxide Hydrolase

In the article, we firstly designed and synthesized a novel fluorescent probe3-epoxy-butyl-6-methyl fluorescein, and its sensitivity and specificity were studied.First, this thesis designed and prepared a novel fluorescent probe using fluorescein as fluorphore. Further experiments showed that the probe has a high sensitivity and good specificity, and could be used for rapid screening of inhibitors of epoxide hydrolase.Second, starting from sodium thiocyanate, acyl thiourea and acyl isothioc-yanate were obtained in good yields by the esterification of isothioc-yanate, followed by nucleophilic addition with amines.Third, starting from benzoyl chloride, phenyl isocyanate and carbamate were obtained in good yields by esterification isocyanate, followed by nu-cleophilic addition with addition with alcohols or phenols. Finally, the new type of fluorescent probe was used to detect the activ-ity of EH, and the inhinbitory of the synthetic compounds towards EH was detected. The results show that compounds have inhibitory effect. For exam ple, compounds3-17(IC50=1.12μM) and3-33(IC50=1.01μM) showed potent inhibition on EH. Experiments of inhibition bacterial for the selected comp ounds were carried out. The sizes of inhibition zone of compounds3-1(21m m),3-25(23mm) showed good inhibitory effect.