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새로운 N-치환 benzotriazol-1-yl유도체의 항균활성에 미치는 치환기 효과
유성재,성민규,김대황,성낙도,Yu, Seong-Jae,Sung, Min-Gyu,Kim, Dae-Whang,Sung, Nack-Do 한국응용생명화학회 1997 Applied Biological Chemistry (Appl Biol Chem) Vol.43 No.1
일련의 새로이 합성된 chira핀 N-치환 benzotriazol-1-yl유도체들의 구조와 잿빛 곰광이균(Botrytis cinerea), 배 검은 무늬병균(Alternaria kikchiana) 및 고추 역병균(Phytophthora capsici) 등 3종의 곰광이균류에 대한 항균활성에 미치는 치환기의 효과를 검토한 결과, 전자끌게(${\sigma}_I$,Y>0)로써 phenoxy 또는 thiophenoxy group(X) 보다는 alkyl또는 phenyl group(Y)이 더 큰 영향을 미쳤으며 phenoxy-치환체, 1이 thiophenoxy-치환체, 2보다 높은 항균활성을 나타내었다. 항균활성에 영향을 미치는 요인으로는 소수성(${\Sigma}logP$)과 유도효과(${\sigma}_I$,Y) 및 Van der Waals(${\Sigma}Vw$) 체적(${\AA}^3$) 등 이었으며 chiral성은 활성개선에 기여하지 못하였으나 tribromomethyl-치환체, 1g는 제일 큰 활성을 나타내는 화합물이었다. Series of new chiral N-substituted benzotriazol-1-yl derivatives were synthesized and their fungicidal activities in vitro against gray mold(Botrytis cinerea), black spot(Alternaria kikuchiana) and phytophthora blight(Phytophthora capsici) were measured by the agar medium dilution method. The substituents effects between the fungicidal activities (obs. $pI_{50}$) and a various physicochemical parameters of phenoxy or thiophenoxy group(X) & alkyl or phenyl group(Y) were analyzed by the multiple regression technique. From the analyzed substituent effects, the structure-activity relationship(SAR) equations shows that the antifungal activities depend on the parameters for the optimal molecular hydrophobicity($({\Sigma}logP)_{opt}$), Van der Waals (${\Sigma}Vw$>0) volume(${\AA}^3$) and inductive constant with electron withdrawing group(${\sigma}_I$,Y>0). The activity in affected by the inductive effect (${\sigma}_I$,Y>${\sigma}_g$X) of Y-group rather than the X-group. The phenoxy substituents, 1, showed higher antifungal activity tn the thiophenoxy substituents, 2. For 1, polar substituent constant(${\sigma}^*$) was an important factor in determining the activity. And the tribromomethyl substituent, 1g showed the highest activity against the tee fungi.
살충성 Imidacloprid의 가수분해 반응 메카니즘
유성재,강문성,성낙도,Yu, Sung-Jae,Kang, Moon-Sung,Sung, Nack-Doo 한국응용생명화학회 1997 Applied Biological Chemistry (Appl Biol Chem) Vol.43 No.1
중성과 알카리성의 $45^{\circ}C$, 15%(v/v) dioxane 수용액중에서 살충성 imidacloprid (lUPAC:1-(6-chloro-3-pyridylmethyl)-3-N-nitro-iminoimidazolidine-2-ylideneamine)의 가수분해 반응속도 상수를 측정하고 pH-효과, 용매효과(m=0.04, n=0.30 및 m${\ll}$l), 열역학적 활성화 파라미터(${\Delta}S^{\neq}$=-0.03e.u. 및 ${\Delta}S^{\neq}=16.14\;kcal{\cdot}mol^-$), 반응 생성물 분석등의 결과로부터 반응 속도식($K_{obs}=4.56{\times}10^{-3}[OH^-]$)을 유도하여 특정 염기촉매 반응($K_{OH^-}$)으로 사면체($sp^3$) 중간체인 1-(6-chloro-3-pyridylmethyl)-2-hydroxy-2-imidazolidinylisonitraminate(I)을 거쳐 imidazolidine 고리 열림반응으로 $\beta$-3-(6-chloro-3-pyridylmethyl)aminoethyl-1-nitrourea(III)를 경유한 다음에 1-(6-chloro-3-pyridylmethyl)aminoethyl-1-nitrourea(III)으로 분해되는 일련의 친핵성 첨가-제거($Ad_N-E$) 반응메카니즘을 제안하였다. 그리고 $45^{\circ}C$의 중성(pH 8.0)에서 반감기(t1/2)는 약 4.5개월로 잔류성이 큰 화합물임을 알았다. The rate of hydrolysis of insecticidal 1-(6-chloro-3-pyridylmethyl) -2-nitro-iminoimidazolidine (common name; imidacloprid) have been investigated in 15%(v/v) aqueous dioxane at $45^{\circ}C$. From the kinetics and non-kinetics data such as pH-effect, solvent effect(m=0.04, n=0.30 IT m<<l), thermodynamic parameter(${\Delta}H^{\neq}=16.14kcal{\cdot}mol^{-1}\;&\;{\Delta}S^{\neq}=-0.03e.u.$), rate equation ($k_{obs.}=4.56{\times}10^{-3}[OH^-]$) and analysis of hydrolysis product, 1-(6-chloro-3-pyridylmethyl-2)-imidazolidinon, the hydrolysis mechanism of imidacloprid is proposed that the specific base catalyzed hydrolysis($K_{OH^-}$) through nucleophilic addition-elimination ($Ad_N-E$) mechanism proceed via intermediate, 1-(6-chloro-3- pyridylmethyl)-2-hydroxy-2-imidazolidinylisonitraminate (I) and ${\beta}$-3-(6-chloro-3-pyridylmethyl)aminoethyl-1-nitrourea(III). And the half-life(t1/2) of hydrolytic degradation at pH 8.0 and $45^{\circ}C$ was about 4.5 months.
제초성 Benzenesulfonyl urea계 화합물의 형태와 반응성
유성재,이상호,고영관,성낙도,Yu, Seong-Jae,Lee, Sang-Ho,Ko, Young-Kwan,Sung, Nak-Do 한국응용생명화학회 1996 Applied Biological Chemistry (Appl Biol Chem) Vol.44 No.1
The most stable stereo conformer in non substituted benzenesulfonyl urea, 1 was the II-keto form, which the molecule was intramolecular associated(H-bond) coformer between imide group and N atom on the Pyrimidine ring. The hydrolytic degradation of 2 derivatives were proceeds by nucleophilic addition reaction(p<0) with orbital controlled intermolecular interaction between LUMO with electron donating$(\sigma<0)$ groups of 2 and HOMO of water molecule. N-(4,6-disub. pyrimid ine-2-yl)aminocarbonyl-2-(1,1-dimethoxy-2-fluoro)ethylbenze nesulfonamides,3 and N-(4,6-disub. triazine-2-yl)aminocarbonyl-2-(1,1-d imethoxy-2-fluoro)ethylbenzenesulfonamides,4 we re synthesized and their herbicidal activities in vivo against bulrush (Scirpus juncoides.) were measured by the pot test under the paddy conditions And the structure activity relationships(SAR) were analyzed by the multiple regression technique. The results of the SAR suggested that the 3 and 4 derivatives indicated dependent on the hydrophobicity of the 4,6-disubstituents and the heterocyclo group, where the optimal value $((log\;P)_{opt.}=0.89)$ of hydrophobicity was 0.89. The pyrimidine substituents, 3 showed higher herbicidal activity than the triazine substituents, 4. Among them, 4,6-dimethoxypyrimidine substituent, 3a showed the best herbicidal activity. 제초성 비치환(H) benzenesulfonyl urea 분자, 1은 sulfonyl group 인접의 amino group과 pyrimidinyl group의 N원자 사이에 회합(H-결합)된 형태(II-keto)가 제일 안정하였으며 phenyl 치환$(R_2$ 및 $R_3)$유도체, 2는 전자를 밀수록$(\sigma<0)$ LUMO(ev.)는 음의 값으로 증가하여 물 분자의 HOMO(ev.)사이에 궤도 조절반응(p<0)에따른 전형적인 친핵 반응성을 나타낸다. N-(4,6-이치환-pyrimidine-2-yl)aminocarbonyl-2-(1,1-dimethoxy-2-fluoro)ethylbenzenesulfonamides, 3 및 N-(4,6-이치환-triazine-2-yl)aminocarbonyl-2-(1,1-dimethoxy-2-리uoro)ethylbenzenesulfonamide, 4 유도체의 4,6-이치환기(X 및 Y) 와 헤테로 고리의 변화에 따른 올챙이고랭이(Scirpus juncodies.) 에 대한 제초활성은 소수성$((log\;P)_{opt.}=0.89)$이 가장 큰 영향을 미치는 요인이었다. 또한, pyrimidine-치환체, 3이 triazine-치환체, 4보다 양호한 제초활성을 나타내었으며 dimethoxypyrimidine-치환체, 3a가 가장 큰 제초활성을 보였다.
유성재,신호철,김영섭,이상범,장지근,공명선,장호정,이준영,이영관,Yu, Sung-Jae,Shin, Ho-Chul,Kim, Young-Sup,Rhew, Sang-Burm,Jang, Ji-Geun,Gong, Myung-Seon,Chang, Ho-Jung,Lee, Jun-Young,Lee, Young-Kwan 한국반도체디스플레이기술학회 2006 반도체디스플레이기술학회지 Vol.5 No.2
This paper presents a optimizing algorithm getting through analyzing a image improvement algorithm using retinex theory. Improving a existing retinex theory's slow process speed, our proposal is that it controls a small filter size of surrounding function by comparing with original algorithm. So slow process speed decreased drastically. For filling a short of lighting information by small filter, we also selected gray image as a forth channel. Using the color constancy, we got fast process time like linear color correction and could do comfortable auto color rectification according to other images.
성낙도,유성재,전동주,김대황 ( Nack Do Sung,Seong Jae Yu,Dong Ju Jeon,Dae Whang Kim ) 한국응용생명화학회 1995 Applied Biological Chemistry (Appl Biol Chem) Vol.38 No.1
Post emergence herbicidal activities(pI_(50)) of X-substituted phenylvinylsulfone derivatives(S) in-vivo against rice(Oryza sativa L), Barnyard grass(Echinochloa crus-galli) and Pickerelweed(Monochoria vaginalis Presl) were measured by the pot test under paddy conditions. The (S) showed herbicidal symptom rapidly with lower activity(average pI_(50)= 2.0) as proherbicide, which was excellent tolerance to rice. The structure activity relationships(SAR) were analyzed using such a physicochemical parameters as hydrophobic(π) and molecular orbital(MO) quantity by the multiple regression technique, and discussed with quantum pharmacology. The herbicidal activities were related to the hydrophobic(π) effect of X-substituent and orbital(HOMO & LUMO) energy. In case of Pickerelweed, the effect was rationalized by parabolic function of π constant, where the optimal value of π was 1.10. An increase in hydrophobicity and negative orbital energy by the electron attracting X-substituent may contribute to the herbicidal activity. Based on results proposed from SAR analysis, the mode of herbicidal action could be assumed.
살충성 Imidacloprid의 가수분해 반응 메카니즘
성낙도,유성재,강문성 ( Nack Do Sung,Seong Jae Yu,Moon Sung Kang ) 한국응용생명화학회 1997 Applied Biological Chemistry (Appl Biol Chem) Vol.40 No.1
The rate of hydrolysis of insecticidal 1-(6-chloro-3-pyridylmethyl)-2-nitro-iminoimidazolidine (common name; imidacloprid) have been investigated in 15%(v/v) aqueous dioxane at 45℃. From the kinetics and non-kinetics data such as pH-effect, solvent effect(m=0.04, n=0.30 & m≪ℓ), thermodynamic parameter(△H^*=16.14㎉·㏖^(-1) & △S^*=-0.03e.u.), rate equation (k_(obs.)=4.56×10^(-3)[OH^-]) and analysis of hydrolysis product, 1-(6-chloro-3-pyridylmethyl-2)-imidazolidinon, the hydrolysis mechanism of imidacloprid is proposed that the specific base catalyzed hydrolysis(k_(OH)) through nucleophilic addition-elimination (Ad_N-E) mechanism proceed via intermediate, 1-(6-chloro-3-pyridylmethyl)-2-hydroxy-2-imidazolidinylisonitraminate (Ⅰ) and β-3-(6-chloro-3-pyridylmethyl)aminoethyl-1-nitrourea(Ⅲ). And the half-life(t½) of hydrolytic degradation at pH 8.0 and 45℃ was about 4.5 months.