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Imidacloprid 와 그 유도체들의 살충활성에 미치는 3 - N - 치환기 ( R ) 의 영향
성낙도(Nack Do Sung),강문성(Moon Sung Kang),장해성(Hae Sung Jang),김대황(Dae Whang Kim) 한국응용생명화학회 1996 Applied Biological Chemistry (Appl Biol Chem) Vol.39 No.2
Imidacloprid and a series of the related compounds were synthesized, and influence of 3-N substituents(R) on the insecticidal activities against Brown plant hopper(Nilaparvata lugens) and Green peach aphid(Myzus persicae) were examined quantitatively from the structure-activities relationships(SAR) techniques. The results indicated that the molecular hydrophobicity(π) and inductive substituent constant(σ^*) of substituents(R) at 3-nitrogen position on the imidazolidine ring were important factors. Variations in the potency were parabolically related to the both constants. In case of Brown plant hopper, optimum value of π constant was 0.52, whereas the value of σ^* constant against Green peach aphid was 1.17, respectively. Among them, the strong electron withdrawing groups(σ^*$gt;0) such as methyl and benzenesulfonyl group(7 & 8) showed lower insecticidal activity and non-substituted, 1(imidacloprid) showed the best insecticidal activity. It seems that the intramolecular associated(H-bond) form between 2-N-nitro group and 3-imid group may contribute to the higher insecticidal activity to the both sucking insects. And in aqueous solution, 1 showed higher residual activity below pH 6.0, and the half-life(T_½) was about 6 month at pH 7.0 (ca. k_(obs) : 5×10^(-8) sec.^(-1)) and 45℃.
새로운 Ortho 이치환 Benzenesulfonyl Urea 유도체의 제초활성과 수용액중의 잔류성
성낙도(Nack Do Sung),김용집(Yong Jip Kim),장해성(Hae Sung Chang),김대황(Dae Whang Kim) 한국응용생명화학회 1995 Applied Biological Chemistry (Appl Biol Chem) Vol.38 No.6
The new sixteen herbicidal N-2-(1-hydroxy-2-fluoroethyl)-6-substituted(X)-benzenesulfonyl-N`-4,6-dimethoxypyrimidinyl-2-yl urea derivatives(S) were synthesized and thier herbicidal activities(pI_(50)) in vivo against rice(Orysa Sativa L.), Barnyard grass(Echninochloa orizicola) and Bulrush(Scirpus juncoides) were measured by the pot test under paddy conditions. The structure activity relationship(SAR) were studied using the physicochemical parameters of ortho-substituents(X) and hydrolysis rate constant(logk) and herbicidal activities by the multiple regression technique. The SAR suggested that the herbicidal activities were more dependant on the hydrolysis rate constant(logk$gt;0) than the steric constants (Es$lt;L1(or B₄)$lt;0), small width(B₄) and length(L₁). Among them, halogens(2 & 5), methyl(15) and non(H) substituent(1) showed higher herbicidal activity for weeds which was not tolerent to rise and weeds. The herbicidal activity was increased and the persistency in aqueous solution was decreased by electron donating(σ0$lt;0) groups as ortho-substituent(X). From the relationship equation between herbicidal activity and hydrolysis rate constant, it was assumed that the both reactions would be proceeds with similar process. And the conditions on the ortho substituents to show higher herbicidal activity and the persistency in aqueous solution were also discussed.
성낙도(Nack Do Sung),이상호(Sang Ho Lee),고영관(Young Kwan Ko),김대황(Dae Whang Kim) 한국응용생명화학회 1996 Applied Biological Chemistry (Appl Biol Chem) Vol.39 No.4
A series of the herbicidal N-(4,6-disubstituted pyrimidin-2-yl)aminocarbonyl-2-(1,1-ethylenedioxy-2-fluoro)ethylbenzenesulfonamides, 1 and N-(4,6-disubstituted triazin-2-yl)aminocarbonyl-2-(1,1-ethylenedioxy-2-fluoro)ethylbenzenesulfonamides, 2 were synthesized and their herbicidal activities in-viva against rice(Oryza saliva L.), barnyard grass (Echinochloa crus-galli), bulrush(Scirpus juncoidesi and pickerel weed(Monochoria vaginalis presl.) were measured by the pot test under the paddy conditions. The structure activity relationships(SAR) between the herbicidal activity(pI_(50)) and a various physicochemical parameters of the hetero group and 4,6-disubstituents on the heterocyclic group were analyzed by the multiple regression technique. The SAR suggest that the 4,6-dimethoxypyrimidine substituent. 1a showed selective(△obs.pI_(50)=1.12) and the most highest activity against barnyard grass, which depend on the hydrophobicity(log P$lt;0) of heterocyclo group and moleculuar refractivity((M_R)_(opt.)=14.58 ㎤/㏖) constant of 4.6-disubstituents on the heterocyclic group.
제초성 Flazasulfuron 의 Smile 자리옮김 반응
성낙도(Nack Do Sung),이광재(Gwang Jae Lee),김용집(Yong Jip Kim),김대황(Dae Whang Kim) 한국응용생명화학회 1996 Applied Biological Chemistry (Appl Biol Chem) Vol.39 No.1
A series of the herbicidal pyridylsulfonyl areas, none substitutent. 1-(4,6-dimethoxypyrimidine-2-yl)-3-(2-pyridylsulfonyl) urea, 3 and 3-trifluoromethyl substitutent, 1-(4,6-ctimethoxypyrimidine-2-yl)-3-(3-trifluoromethyl-2-pyridylsulfonyl) urea, 5(Flazasulfuron) were syntbesizied and the rate of hydrolysis of their has been studied in 25%(v/v) aqueous dioxane at 45℃. From the results of solvent effect(m≪, n≪3 & |m|≪|ℓ|), thermodynamic parameter (△S=0.54∼-2.19e.u. & △H=0.025 Kcal.mol.^(-1)), hydrolysis product analysis, pK_a constant(3: 4.9 & 5: lit.4.6) and the rate equation, a marked difference in the kinetics of the reaction of 3 and 5(Flazasulfuron) was observed. It may be concluded that the hydrolysis of 5 proceeds through the A-S_N2Ar reaction via conjugate acid(5H^+) below pH 7.0, whereas, above pH 9.0, the hydrolysis proceeds through irreversibly (E₁)_(anion) and reversibly (E₁CB)_R mechanism via conjugate base(CB), respectively. But in case of 5, A-S_N2Ar, (E₁)anion and (E₁CB)_R mechanism involved Smile rearrangement. The mate of rearrangement of 5 to a 3-trifluoromethyl-2-pyridylpyrimidinyl urea(PPU) in acid and 3-trifluoromethyl-2-pyridyl-4.6-dimethoxypyridinyl amine (PPA) in base was increased about 3.5 times by the introduction of trifluoromethyl group in the 3-position on the 2-pyridyl ring. From the basis of these findings, a possible mechanism for the hydrolysis of 5 was proposed and discussed.
2 - ( n - Octyl ) - 3 - ( n - propyl ) isothiourea 유도체의 살충활성에 미치는 N - 치환 Amino group 의 영향
성낙도(Nack Do Sung),정경채(Kyoung Chae Jeong),전동주(Dong Ju Jeon),김대황(Dae Whang Kim) 한국응용생명화학회 1995 Applied Biological Chemistry (Appl Biol Chem) Vol.38 No.2
New twenty 2-(n-octyl)-3-(n-propyl)isothiourea derivatives(S) were synthesized which is modified from the insedicidal Buprofezine (Applaud) in the selective insecticidal activities in-vitro against Diamond-Back moth (Plutella Xylostella Linnaeus). The structure activity relationships(SAR) between the insecticidal activity(pI_(50)) and a various physicochemical parameters of the substituent(Z) of S were analyzed by the multiple regression technique. The activities would depend largely on the MR, π and L₁ parameters. The SAR was rationalized by parabolic function of MR, π, and L₁ constant, where the optimal values of the constants were L₁= 5.22 Å, MR=15.70 C㎥/㏖ and π=1.60, respectively. The steric effects play an important role in determining insecticidal activity. The SAR suggest that the S derivatives having a substituents with a small breadth and an appropriate length as Z group showed potent activity. From the results, the iso-propyl group(Z) substituent (5) with three carbon atom was the most effective compound.