Study On Synthesis And Their Mechaanism Of 22 Plant Pathogenic Fungi Inhibitors

Chalcone and its derivatives are products of aromatic aldehydes and ketones cross aldol condensation of 1,2-phenyl ketone two propylene.It is the parent compound is the precursor substance of Plant Flavonoid Biosynthesis and the product directly from the natural resources（such as acquisition of liquorice,safflower and other natural plant）,with high safety,both nutrition and medicinal effects.In recent years,studies on chalcone compound antibacterial activity of a large number of reports,but the water soluble and fat soluble are poor,low bioavailability,limiting the its application in clinic.Therefore,it is necessary to modify and modify its structure in order to get more active,less toxic and new structure.The study of 22 kinds of medicine,isophorone derivatives synthesis and identification of;Study on antibacterial activity of synthetic material;antibacterial mechanism of.The paper is studied from the following three aspects.1.Synthesis and identification of Isophorone derivativesObjective:To synthesize 22 novel derivatives,seoul.Methods:to acetophenone and thiophene-formaldehyde as the main raw material by Claisen Schmidt condensation reaction,in ice water bath temperature control conditions,in dilute NaOH ethanol solution under the condition of synthesis of a series of laboratory isophorone derivatives.They were characterized by IR,1H NMR structure is confirmed.Results:22 kinds of pure substances were synthesized.Conclusion:through the structural analysis,the pure substance is determined as the target material.2.Synthesis and identification of Isophorone derivativesObjective:to preliminarily screen the inhibitory effect of synthetic substances on the plant pathogenic fungi,so as to lay a foundation for the development of new fungicides with high efficiency,low toxicity and safety.Methods:the plate growth rate method for determination of medicine,isophorone substance of ten kinds of common plant pathogenic fungi:Citrus green mold,Fusarium graminearum,grape white rot fungus,Sclerotinia bacteria,melons anthrax,rice sheath blight,apple ring rot pathogen,Bipolaris maydis,potato potato late blight,tomato gray mold bacteria indoor antimicrobial effect.The antibacterial results:Good inhibitory effect against Gibberella zeae,the inhibition of growth for1^#、6^#、7^#、8^#、10^#、11^#reached60.0%at a concentration of 100 mg L^-1,respectively.Good inhibitory effect against Coniothyrium diplodiella（Speg.）Sacc,the inhibition of growth for2^#、7^#、19^#、22^#and 12^#reached60.0%at a concentration of 100 mg L^-1,respectively.Good inhibitory effect against Sclerotiua sclerotiorum,the inhibition of growth for1^#、2^#、7^#、8^#、9^#、10^#、11^#、12^#、13^#、14^#、15^#、18^#、19^#、20^#、21^#reached 60.0%at a concentration of 100 mg L^-1,respectively.Median effective concentrations(EC₅₀)of 7^#reached 22.98mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9126.Chisquare test demonstrated that the results were reliable（c²=2.419,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of 8^#reached 10.12mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9357.Chisquare test demonstrated that the results were reliable（c²=0.078,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of 11^#reached 39.63 mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9105.Chisquare test demonstrated that the results were reliable（c²=0.524,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of18^#reached 21.31 mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was0.9563.Chisquare test demonstrated that the results were reliable（c²=0.357,df=3,p（29）0.05）.Good inhibitory effect against Coniothyrium lagenarium,the inhibition of growth for2^#、5^#、7^#、12^#、13^#、14^#、22^#reached 60.0%at a concentration of 100 mg L^-1,respectively.Median effective concentrations(EC₅₀)of 2^#reached 33.21mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9503.Chisquare test demonstrated that the results were reliable（c²=1.737,df=3,p（29）0.05）.Good inhibitory effect against Rhizoctonia solani,the inhibition of growth for1^#、2^#、6^#、9^#reached 60.0%at a concentration of 100 mg L-¹,respectively.Good inhibitory effect against Physalospora piricola,the inhibition of growth for2^#、7^#、13^#、14^#reached60.0%at a concentration of 100 mg L^-1,respectively.Median effective concentrations(EC₅₀)of13^#reached 10.10mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was0.9448.Chisquare test demonstrated that the results were reliable（c²=1.090,df=3,p（29）0.05）.Good inhibitory effect against Helminthosporium maydis,the inhibition of growth for6^#、7^#、8^#、9^#、10^#、11^#、12^#、13^#、15^#、16^#、17^#、18^#、19^#、22^#reached 60.0%at a concentration of 100 mg L^-1,respectively.Median effective concentrations(EC₅₀)of 9^#reached 21.40mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9419.Chisquare test demonstrated that the results were reliable（c²=0.245,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of 10^#reached 21.00mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9379.Chisquare test demonstrated that the results were reliable（c²=0.097,df=3,p（29）0.05）.Good inhibitory effect against Phytophthora infestans,the inhibition of growth for2^#、12^#、14^#、22^#reached 60.0%at a concentration of 100 mg L^-1,respectively.Good inhibitory effect against Botrytis cinerea,the inhibition of growth for2^#、5^#、6^#、7^#、8^#、9^#、10^#、11^#reached 60.0%at a concentration of 100 mg L-¹,respectively.Median effective concentrations(EC₅₀)of 6^#reached 31.91 mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9539.Chisquare test demonstrated that the results were reliable（c²=0.294,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of 7^#reached 44.90 mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was0.9506.Chisquare test demonstrated that the results were reliable（c²=1.171,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of 8^#reached 42.69 mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9422.Chisquare test demonstrated that the results were reliable（c²=0.9422,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of 10^#reached 31.47 mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9602.Chisquare test demonstrated that the results were reliable（c²=1.013,df=3,p（29）0.05）.Median effective concentrations(EC₅₀)of 11^#reached 21.17 mg L^-1The results of regressive and correlative analysis indicated that the correlation was significant between concentration and efficacy.Its correlative coefficient was 0.9363.Chisquare test demonstrated that the results were reliable（c²=0.181,df=3,p（29）0.05）.Conclusion There are a lot of compounds which have good antibacterial effect against these common pathogenic fungi.These compounds wree developed as highly efficient and low toxicity and safety of new fungicide is feasible.3.Preliminary study on the mechanism of inhibiting plant pathogenic fungiThe reaction between Bovine Serum Albumin（BSA）and 1-（3-chlorphenyl）-3-（thiophen-2-yl）-prop-2-en-1-one was studied through the methods of Synchronous fluorescence,UV absorption and fluorescence quenching in the simulated physiological conditions in this paper,as well as the effect of common metal ions(Cu²⁺、Cd²⁺、Hg²⁺、Co²⁺、Ag⁺、Pb²⁺)on the TU-BSA system.The results show that the intrinsic fluorescence of BSA was decreased with the increase of the concentration of TU under simulating physiological condition,and the quenching mechanism is a static quenching process.The binding constants between TU and BSA at 293 K、299 K、310 K were 3.09×10⁵ L·mol^-1、2.60×10⁵ L·mol^-1、2.13×10⁵ L·mol^-1,respectively.The values of the thermodynamic parameters（ΔG/ΔH/ΔS）were calculated according to the thermodynamic equation.The thermodynamic parameters indicated that binding process between TU and BSA was spontaneous,and the hydrophobic force played an important role on the conjugation reaction.According to the data of F?rster’s non-radiative energy transfer theory,the conjunct distance between BSA and TU was 1.86 nm.The binding of TU to BSA was weakened in presence of Cu²⁺,Cd²⁺,Hg²⁺,Co²⁺,Ag⁺,while increased in presence of Pb²⁺.