Synthesis And Biological Activity Of Indazole Derivatives

As an important subunit in drugs,the indazole has been used widespread in medic ine,such as anti-HIV,anti-tumor,and anti-inflammatory.But there are not so many reports about the use of the indazole compounds in pesticides.In this paper,novel indazole derivatives were designed and synthesized by means of random synthesis and analogue synthesis,their spectrum properties,insecticidal activities, fungicidal activities,herbicidal activities and their structure-activity relationship were studied meanwhile.What the paper studied may be summarized as follows:1.In this paper,the research progress of both the nitrogen-containing heterocyclics (pyrazoles,pyrroles and pyridines)and nitrogen-containing fused heterocyclics (indazoles and so on)with biological activities were reviewed,their commercialized products were introduced in detail,mechanisms of action and applications in agriculture of some commercialized products were also explained.2.Thirty-seven compounds in three series were designed and synthesized.The structure of all these compounds were confirmed by GC-Mass,LC-Mass,¹H NMR and IR.These compounds can be summarized as follow:(â… )1H-indazole(6).(â…¡)1H-indazole-4(7)-carboxylate(24).(â…¢)1H-indazole-4(7)-carboxamide(7).3.The synthesis methods and possible mechanisms of the indazoles were explored.4.Insecticidal activities,fungicidal activities and herbicidal activities of synthesized compounds were studied,the bioassay data indicated that some compounds possessed remarkable insecticidal or fungicidal activities.For example,compoundsâ…¡₉ andâ…¢₇ showed large than 90.0%insecticidal activity against Nephotettix cincticeps at 500 mg/L, and compoundsâ…¡₃,â…¡₂₄andâ…¢₂ exhibited large than 90.0%fungicidal activity against Erysiphe graminis at 500 mg/L.