Studies On Synthesis And Fungicidal Activity Of Inhibitior Of Ergosterol Biosynthesis

The development of traditional chemical pesticides has been limited because of traditional chemical pesticides having been some harm to human health,environment and non-target organism,so the creative direction of present new pesticide creative direction has been becoming to look for the new high performance,lower toxicity,good selectivity and higher safety fungicide。Triazole compounds attracted people's more concern because of broad-spectrum of biological activity,lower toxicity,lower resistance and the diversity of chemical structural。3,3-dimethyl-1-(-1,2,4-1-trizole-1-yl)-butanone is an important intermed- iate which synthesize triazole fungicide,and most of their prepared derivatives have good fungicidal activity。At present, many products have been developed and applied such as fungicides, insecticides,plant growth regulator and drugs。Triazole compound of different structures has different biological activity, so the new structures of triazole compound's research and development becomes a hotspot。The paper researched the biosynthesis pathway of Ergosterol,the key enzymes of biosynthesis of ergosterol,the action mechanism of active group and structure-activity relationship。Eight novel triazole compounds which target enzyme were squalene epoxidase and isomerase/reductase and which raw material was 3,3-dimethyl-1-(-1,2,4-1-trizole-1-yl) - butanone was synthesized by aldehyde-ketone condensation,Michael addition reaction and reduction reaction。The structure of compounds was identified by IR,1H NMR,13CNMR and MS spectral methods.The antifungal activity of compounds were performed。The results showed that at the concentration of 100 mg/L,all of compounds showed different activity against four plant pathogenic fungi。The inhibition rate of compound 2 to four plant pathogenic fungi is higher than other compounds and more than 70%,especially to Cotton Fusarium Wilt。The inhibition rate of compound 3 to four plant pathogenic fungi is lower than other compounds,especially to Fusarium graminearum and Fusarium oxysporium,6.08% and 4.41% respectively。The inhibition rate of the compounds expect for compounds 3 to Cotton Fusarium Wilt is higher than other plant pathogenic fungi。The inhibition rate of compound 3 to Fusarium oxysporium which is 71.57% is higher than to other plant pathogenic fungi。...