Studies On Synthesis And Bioactivity Of Novel Uracil Compounds

Uracil derivatives and the phenoxy carboxylic acid have important biological activities. Uracil compounds are one kind of highly active protoporhyrinogen oxidase (Protox) inhibitors. this herbicides take photosynthesis as it's object,which insures the special toxicity on the title plant from the animals.The phenoxy carboxylic acid derivatives have extensive application and the research values in the agriculture, forestry and environment.The latest research and development of herbicide and protox inhibitors were reviewed in this article. We also present the latest progress on 3-aryl uracil derivatives, including their structures, research process, synthetic methods, bioactivities, along with prospects and trends for future development of uracil derivatives. Otherwise, The latest research and development of the phenoxy carboxylic acid derivatives in pesticide were introduced in detail.We reasonablly combined with uracil derivatives and the phenoxy carboxyl acid which have different action mechanism, 37 new compounds weresynthesised by me too designing principles such as sub-structure linkage and bioisosterism. Their structures were confirmed by IR, ~1H NMR and LC/MS.According to their structures, these compounds can be divided into two series as following:(1)N-(2-substituted-4-chloro-5-(3-methyl-2,6-dioxo-4-(trifluoromethyl)-2,3-dihydropyrimidin-1(6H)-yl)phenyl)-2-substituted benzoxyacetamides(benzoxypropanamides)â… :(2)N-(2,4-disubstituted-5-(3-methyl-2,6-dioxo-4-(trifluoromethyl)-2,3-dihydropyrimi din-1 (6H)-yl)phenyl)-2-substituted benzoxyacetamides (benzoxypropanamides),â…¡: (3)N-(3-(5-chloropyridin-2-yl)-6-(trifluoromethyl)-1,2,3,4-tetrahydro-1-methyl-2,4-dioxopyrimidin-5-yl)propanamide -2-substituted benzoxyacetamides (benzoxyproanamides )â…¢:Some of compoundsâ… ,â…¡were tested for herbicidal activity. It was found that these compounds showed different herbicidal activity by post-emergence treatment and pre-emergence treatment. The herbicidal activity on dicotyledon weeds is better than on monocotyledon weeds. Some of the compounds exhibited 100% inhibition to dicotyledon weeds at 75 g a.i./hm~2, such as Abutilon theophrasti, Amaranthus spinosus by post-emergence treatment. The bioassay of Some of compoundsâ… ,â…¡and compoundsâ…¢is underway.At the same time, compounds were tested for bactericidal activity and isecticidal activity. It was found that some of compounds showed different bactericidal activity and isecticidal activity.