Synthesis And Biological Activity Testing Of Pyridine-containing Bisamide Derivatives

Bisamide insecticides have a unique mechanism of action,high efficiency,low toxicity,and no cross resistance to exist pesticides and other characteristics of popular favor researchers.The drug trades successfully developed had flubendiamide,chlorantraniliprole,cyantraniliprole.In order to develop a highly active compound and create security,economic,friendly drugs,the paper treated chlorantraniliprole as a precursor compound,then pyridyl pyrazole partially was replaced by pyridine.On the one hand,on the pyridine ring introducing active fragment containing the N series obtained 14 target compounds;on the other hand,the pyridine-containing intermediate condensation,then introduced active fragment containing the N series to obtain 14 target compounds.All of the target compounds were adopted by IR,¹H NMR,¹³C NMR,MS characterization.All target compounds were tested antibacterial activity on Xanthomonas oryzae,Tobacco Ralstonia bryoniae,Xanthomonas citri at 200?g/m L and 100?g/m L.Preliminary antibacterial activity tests showed that some target compounds have a some inhibitory activity on the three bacterias.Wherein,the inhibition rates of compounds C-08,Q-08,Q-09 at 200?g/m L on Tobacco Ralstonia bryoniae were86.0%,86.5%,79.7%,higher than the control agent Bismerthiazol.At the concentration of 100?g/m L,respectively,the inhibition rates were 14.9%,48.2%,24.9%.At the concentration of 200?g/m L,The inhibition rates of Compounds C-06,Q-03,Q-08,Q-13,Q-14 on Xanthomonas citri were above 70%,the inhibition rate were respectively 76.8%,74.1%,73.5%,94.0%,90.0%.At the concentration of 100?g/m L,The inhibition rates of Compounds C-06,Q-03,Q-08,Q-13,Q-14 were respectively 32.0%,47.0%,28.4%,75.0%,68.9%.It was worth noting that inhibition rate of the compound Q-13,Q-14 were higher at the concentration of 200?g/m L and100?g/m L on Xanthomonas citri than the control agent.Using in vitro growth rate method,selected better inhibitory activity against bacteria of the target compound to test Gibberella zeae,Botrytis cinerea and Eggplant wilt fungus germs.Three preliminary activity screening results showed that the test compounds had some antibacterial activity on Gibberella zeae,Botrytis cinerea and Eggplant wilt fungus germs at 50?g/m L.The inhibition rates of the compound Q-03on Gibberella zeae was more than 50%.The inhibition rate of Compounds C-13,Q-09,Q-13 on Botrytis cinerea were more than 40%,respectively,46.04%,49.36%,41.25%.The inhibition rate of compound Q-03 on Eggplant wilt fungus germs reached more than 50%.