Synthesis And Biological Activity Test Of Indole-1, 2, 3-substituted Derivatives

Rencently,indole compounds have drawn much attention due to their extensive biological activity and active sites,making them one of the hot topics in the research of new pesticide and new medicine innovation.In order to innovate higher efficient antitumor and antibacterial compounds,with oxindole as the lead compound,A series of indole hydrazones were designed and synthesized.Synthesis of target compounds were verified by HRMS,¹H NMR,¹³CNMR characterization and melting point test was carried out.Of all target compounds using the turbidity method,the antibacterial activity test.Synthesized compounds respectively to rice bacterial leaf blight fungus,tobacco solanacearum,citrus canker bacteria,a total of three bacteria bacteriostatic activity screening.The preliminary bioassay results indicated that all of the title compounds exhibited a certain antibacterial activities in vitro against Xanthomonas oryzae pv.oryzae,Ralstonia.solanacearum and Xanthomonas axonopodis pv.Citri.These title compounds M₄、M₈、M₉、M₁₄4 and M₁₇7 displayed good antibacterial activities against the above three plant pathogenic bacteria.the concentration of 50%inhibition rate(EC₅₀)of M₄、M₈、M₉、M₁₄4 and M₁₇7 against X.oryzae were 73.79,61.94,59.70,36.72and 82.79μg/mL,which was significantly superior to the control bismerthiazol and thiodiazole-copper（92.46μg/mL and 120.22μg/mL,respectively）.Anticancer activities of the target compounds against Hela and HepG2 were tested by the MTT method.The results showed that some compounds had some inhibitory effects on Hela cells,of which M₁₄4 had the best inhibitory effect on Hela cells,which was better than that of gefitinib,The inhibitory effect on HepG2 is poor;the inhibitory effect of M₁₇7 on Hela cells and HepG2 cells is relatively good.