Chemical Modification And Antibacterial Performance Of Fluconzole

Triazole is an inhibitor of ergo sterol biosynthesis, is widely used in medicine, pesticides, wood preservation in other fields. And is favored because of its broad-spectrum, high efficiency, low toxicity, etc. In this paper, To study the ergo sterol biosynthetic pathway, and to understand the mechanism of action of triazole. Nine1,2,4-triazole compounds were designed and synthesized and through Antibacterial experiments, active compounds were selected. The details are as follows:1Compounds Y-4(a-i) were obtained from the1,3-two chlorobenzene by the following methods:Friedel-crafts Acetylation, Alkylation, Epoxidation, and ring opening. The structures of these compounds were certified by MS and1H-NMR. and synthesis conditions are mild and easy, so they have a value.2The optimization of alkylation has been done, namely, That temperature, time, solvent, acid-binding agent, the Raw materials ratio have been Experimented Respectively; Last, the best process is selected, That is toluene as a solvent, triethylamine as acid-binding agent, reaction time6h, Raw materials ratio n (Y-1):n (1,2,4-triazole)=1:1.8, reaction temperature is90℃. This way Simplify the experimental conditions and increase the the yield.3Making the mass fraction of target compound solution were0.5%,1.0%,1.5%,2.0%. Then antifungal activities of these compounds were evaluated by two moulds and two decay fungi with Filter paper diffusion, The outcome show that Y-4e、4g has a inhibitory effect on Aspergillus niger, All target compounds has no effect on Trichoderma viride, but all have a certain effect on Coriolus versicolor and Gloeophyllum trabeum. And antibacterial activity will be increasing by concentration enhancement, Where Y-4i theory has a certain value.