Design?synthesis And Herbicide Activity Of Novel Diketonitrile Derivants Of Hppd Inhibitors

4-Hydrooxyphenylpyruvate dioxygenase(HPPD)is a kind of target enzyme in resent year.HPPD can be found in a series of organisms.In the plant,it catalyses the synthesis of tocopherol.That is to say it turns 3-(4-hydroxyphenyl)-2-oxopropanoic acid(HPP)into 2-(2,5-dihydroxyphenyl)acetic acid(HGA).Herbicide will combine with 4-hydrooxyphenylpyruvate dioxygenase completely.As a result,it will interfere in the synthsis of tocopherol and carotenoid indirectly.Eventually the meristematic tissue of plant will die of albino.HPPD inhibitor can be widely used before planting or after seeding.HPPD is traditionly famous for high activity,less-persistence,environmental friendly and safty uses.So it becomes an important target enzyme after ALS,ACC and PPO.Now many researchers are interested in it and it is one of the hot spots in pesticide study.According to the study of papers and research,we combine quionline and furan/thiophene with diketonitriles to get the new HPPD inhibitors on the foundation of the study of our research group.And successfully get two kinds new HPPD inhibitors which are 42 in total.All of the taget compounds are characterized by NMR,mass spectrometry and elemental analysis.The biological activity of these compounds is also been studied preliminarily.According to the result of biological,we can see that several kinds of the new compounds show herbicidal activities.And the Ki of it is as high as 0.0034?M which lower than the Ki(?M)of mesotrione which is the commercial herbicide of HPPD.Some compounds also show herbicidal activities in vivo.For example YJ15161 has a high activity(above 90%)over broadleaf weeds mustard,chickweed,small pigweed,which is currently being further dose screening.