• Title/Summary/Keyword: Control Derivatives

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Influence of substituted phenylcarbamoyl group on the fungicidal activites of a new 5,6-dihydro-2-trifluoromethyl-1,4-oxathiincarboxanilide derivatives (새로운 5,6-dihydro-2-trifluoromethyl-1,4-oxathiincarboxanilide 유도체의 항균활성에 미치는 치환-phenylcarbamoyl group의 영향)

  • Sung, Nack-Do;Yu, Seong-Jae;Nam, Kee-Dal;Chang, Kee-Hyuk;Hahn, Hoh-Gyu
    • The Korean Journal of Pesticide Science
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    • v.2 no.3
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    • pp.64-69
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    • 1998
  • New thirty derivatives of 5,6-dihydro-2-trifluoromethyl-1,4-oxathiin carboxanilide as substrate(S) were synthesized and their fungicidal activities in vivo against rice sheath blight(Rhizoctonia solani) and wheat leaf rust(Puccinia recondita) were examined. The structure activity relationships(SAR) between the activities($pI_{50}$) and a physicochemical parameters of substituents(X) at the phenylcarbamoyl group were analyzed using the adaptive regression analysis method. The 3-methoxy, 11, 3-isopropyloxy, 13 and 3-isopropyl substituent, 25 as X on the phenylcarbamoyl group exhibited the most highest fungicidal activity against the two fungi. The fungicidal potency of the (S) against Puccinia recondita was higher than Rhizoctonia solani. In case of Rhizoctonia solani, the molecular hydrophobicity(${\pi}>0$) and resonance effect(R<0) by meta-alkyl substitutents with electron donating were important factors in determining fungicidal activity. And the HOMO energy(HOMO>0), ABSQ, sum of absolute values of the atomic charges on each atom and specific polarizability(Sp.Pol<0) of (S) were significantly influential towards fungicidal activity against Puccinia recondita.. The interaction between (S) and receptor agonist from the based on SAR studies proceeds through charge-control reaction, and conditions to show higher activity has been also discussed.

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Hydrolytic Reactivity and Holographic Quantitative Structure-Activity Relationship Analyses on the Melanogenesis Inhibitory Activities of Alkyl-3,4-dihydroxybenzoate and N-Alkyl-3,4-dihydroxybenzamide Derivatives (Alkyl-3,4-dihydroxybenzoate와 N-Alkyl-3,4-dihydroxybenzamide 유도체들의 가수분해 반응성과 멜라닌 생성 저해활성에 관한 홀로그램(H) QSAR 분석)

  • Sung Nack-Do;Jung Hoon-Sung;Kim Sang-Jin
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.4 s.48
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    • pp.491-497
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    • 2004
  • Holographic quantitative structure activity relationships (HQSAR) between the melanogenesis inhibitory activities of alkyl-3,4-dihydroxybenzoate (A) and N-Alkyl-3,4-dihydroxybenzamide (B) derivatives were analyzed and discussed. The statistical results of HQSAR model for the activities showed the best predictability of the activities based on the cross-validated $r^2_{cv}\;(q^2=0.674),$ non-cross-validated, conventional coefficient $(r^2_{ncv}=0.936).$ The melanogenesis inhibitory activities and hydrolytic reactivity of (A) were slightly higher than that of (B) (A>B) and the activities depends upon the $R_1-substituents\;(R_1>R_2).$ It has been found using frontier molecular orbital (FMO) theory that the hydrolysis reactions of (A) and (B) proceeded to an orbital-controlled reactions, while the nucleophillc addition-elimination reactions $(Ad_{N-E})$ between LUMO energy of (A) and (B) and HOMO energy of water molecule are occurred.

Effects of Type and Level of Forage Supplementation on Voluntary Intake, Digestion, Rumen Microbial Protein Synthesis and Growth in Sheep Fed a Basal Diet of Rice Straw and Cassava

  • Premaratne, Sujatha;van Bruchem, J.;Chen, X.B.;Perera, H.G.D.;Oosting, S.J.
    • Asian-Australasian Journal of Animal Sciences
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    • v.11 no.6
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    • pp.692-696
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    • 1998
  • An experiment was conducted with eight growing sheep (average initial weight 20.6 kg and average final weight 23.7 kg) in a $4{\times}4$ Latin square design to study the effect of type of forage supplementation to a basal diet of rice straw (ad libitum) and cassava (Manihot esculanta, approximately 9 g of dry matter $(DM).kg^{-0.75}{\cdot}day^{-1}$) on voluntary intake, digestion, rumen microbial protein synthesis and daily weight gain. Forages used were Leucaena (L, Leucaena leucocephala), Gliricidia (G, Gliricidia maculata) and Tithonia (T, Tithonia diversifolia, wild sunflower) at a DM supplementation level of approximately $13g.kg^{-0.75}.day^{-1}$. Organic matter intake was 40.4, 55.5, 55.0 and $54.9g{\cdot}kg.^{-0.75}{\cdot}day^{-1}$ for control (C, ad libitum straw and cassava), L, G and T. respectively, significantly lower for C than for the supplemented diets. Intake of supplementary forage had also a significantly positive effect on voluntary rice straw intake. All forage supplemented diets showed a significantly higher whole diet organic matter digestion than C ($488g{\cdot}kg^{-1}$), while T ($557g{\cdot}kg^{-1}$) differed significantly from L ($516g{\cdot}kg^{-1}$) but not from G ($526g{\cdot}kg^{-1}$). Daily weight gain was -1.7, 5.2, 5.4 and $4.7g{\cdot}kg^{-0.75}$, for C, L, G and T. respectively, significantly lower for C than for the forage-supplemented diets. Efficiency of microbial protein synthesis estimated from urinary excretion of purine derivatives was lower for C (3.8 g microbial N. (kg digestible organic matter intake $(DOMI))^{-1}$ than for the forage supplemented diets (11.3, 9.0 and 9.4 g microbial $N.(kg\;DOMI)^{-1}$ for L, G and T. respectively).

N-phenyl Substitutent Effect on the Herbicidal Activity of 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenylpropionamide Derivatives against Rice Plant with Pre- and Post-emergence (발아 전 후 벼의 약해에 미치는 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenylpropionamide 유도체들 중 N-phenyl치환기의 효과)

  • Lee, Sang-Ho;Ryu, Jae-Wook;Woo, Jae-Chun;Koo, Dong-Whan;Kim, Dae-Whang;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.43 no.1
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    • pp.52-56
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    • 2000
  • The influence of the 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenyl- propionamide derivatives on the herbicide activities against rice plant with pre-emergence and post-emergence in down land were examined and the structure activity relationship (SAR) were analyzed by Free-Wilson and Hansch method. In pre-emergence, the SAR approach is shown that the optimal, $({\pi})_{opt}=0.91$, hydrophobicity with electron donating effect of the ortho substituted mono substituents and 2,3,4-substituted three substituents were found to be contribute the herbicidal activity. Whereas, in post-emergence, the optimal, ({\pi})_{opt}=0.50$, hydrophobicity with electron withdrawing effect of meta substituted mono subsituents and 2,3-substituted two substituents were found to be contribute the herbicide activity. The herbicide activities with post-emergence more increase than that of pre-emergence. It is assumed from the SAR equations that the 2-methyl-3-methoxy-4-cyano group substituent is selected as the most lowest herbicide activity against rice plant with post-emergence in green house. The hydrolysis reaction was proceeded through nucleophilic addition-elimination (Ad_{Nu-E})$ with the orbital control between LUMO of substrate and HOMO of water molecule. And molecular electrostatic potential (MEP) of none (H) substituent was discussed.

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Synthesis of Chloroacetamide Compounds and their Herbicidal Activities (Chloroacetamide형(型) 화합물(化合物)의 합성(合成)과 제초활성(除草活性))

  • Hong, Moo-Ki;Jeong, Young-Ho;Oh, Se-Mun
    • Applied Biological Chemistry
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    • v.31 no.3
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    • pp.234-240
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    • 1988
  • Some chloroacetamide derivatives were synthesized from 2,6-dialkyl, aniline 4-chloroaniline, or 3,4-dichloroaniline with alkyl 2-bromopropionate and chloroacetyl chloride and identified by elemental analyses, NMR, and GC/MS spectra as N-(1'-methoxycarbonylethyl)-N-chloroacetyl-2,6-dimethylaniline(ACRI-S-8609), etc. These compounds synthesized were subjected to the test for pre-emergence herbicidal effecs on some grass weeds(Digitaria adscendens, Setaria viridis, Echinochloa crus-galli) and broad leaf weeds(Portulaca oleracea, Amaranthus lividus, Chenopodium album) in pots applied as wettable powder formulations. It was found that N-(1'-ethoxycarbonylethyl)-N-chloroacetyl-2,6-dimethylaniline(ACRI-S-8701) has the highest herbicidal effect on grass weeds, which corresponds to a 95% control effect at an application of 200g a.i/10a. Whereas, some chloroacetamide derivatives derived from 4-chloroaniline or 3,4-dichloroaniline had very weak herbicidal effects on grass and broad leaf weeds.

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The Search of Pig Pheromonal Ordorants for Biostimulation Control System Technology: IV. Comparative Molecular Similarity Indices Analyses (CoMSIA) on the Binding Affinities between Ligands of 2-(Cyclohexyloxy)-tetrahydrofurane Derivatives and Porcine Ordorant Binding Protein (생물학적 자극 통제 수단으로 활용하기 위한 돼지 페로몬성 냄새 물질의 탐색: IV. 2-(Cyclohexyloxy)tetrahydrofurane 유도체와 Porcine Odorant Binding Protein 사이의 결합 친화력에 관한 비교분자 유사성 지수분석(CoMSIA))

  • Sung, Nack-Do;Park, Chang-Sik;Jang, Seok-Chan;Choi, Kyung-Seob
    • Reproductive and Developmental Biology
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    • v.30 no.3
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    • pp.169-174
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    • 2006
  • To search of a new porcine pheromonal odorants, the comparative molecular similarity indices analysis(CoMSIA) between porcine odorant binding protein(pOBP) as receptor and ligands of green odorants 2-(Cyclohexyloxy)tetrahydrofurane derivatives as substrate molecule were conducted and disscused quantitatively. In the optimized CoMSIA model(I-AI) with chirality($I:\;C_{1'}(R),\;C_2(S)$) in substrate molecules and atom based fit alignment(AE) of the odorants the statistical PLS results showed the best predictability of the binding affinities based on the LOO cross-validated value ${r^2}_{cv.}\;(q^2=0.856)$ and non cross-validated conventional coefficient(${r^2}_{ncv.}=0.964)$). The structural distinctions of the highest active molecules were able to understand from the interaction between pOBP and green odorants in the contour maps with CoMSIA model.

Acaricidal and antimicrobial toxicities of Cyanachum paniculatum root oils and these components against Haemaphysalis longicornis and human intestinal bacteria (산해박 뿌리에서 추출한 정유 및 구성성분의 인간 장내미생물에 대한 항균활성 및 작은소피참진드기에 대한 살비활성)

  • Lee, Myung-Ji;Kim, Hui-Ju;Jeong, Ah-Hyeon;Lee, Hoi-Seon
    • Journal of Applied Biological Chemistry
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    • v.61 no.4
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    • pp.423-428
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    • 2018
  • Anaerobic growth-inhibiting and acaricidal activities of 2'-hydroxy-5'-methoxyacetophenone derived from Cyanachum paniculatum oil and its derivatives against five intestinal bacteria (Bifidobacterium bifidum, B. longum, Clostridium pefringens, Escherichia coli and Lactobacillus casei) and Haemaphysalis longicornis were examined. In the packet test against the larvae of H. longicornis, none of the C. paniculatum oil exhibited acaricidal activity, while the C. paniculatum oil showed only antimicrobial activity against five intestinal bacteria in the disc diffusion method. Based on the inhibition zones and MIC values, 2',4'-dimethoxyacetophenone, 2',5'-dimethoxyacetophenone, 2'-hydroxy-4'-methoxyacetophenone, 2'-hydroxy-5'-methoxyacetophenone, 2'-methoxyacetophenone, and 4'-methoxyacetophenone, containing a methyl group on the acetophenone skeleton, possessed growthinhibiting activities against C. perfringens and E. coli. However, acetophenone, 2'-hydroxyacetophenone, 4'-hydroxyacetophenone, 2',4'-hydroxyacetophenone and 2',5'-hydroxyacetophenone, which contained a hydroxyl group on the acetophenone skeleton, had no growth-inhibiting activity against intestinal bacteria. These results indicated that 2'-hydroxy-5'-methoxyacetophenone and its derivatives could potentially be developed as natural antimicrobial agents to specific control of C. perfringens and E. coli.

Effect of administration with fat-free diet and dietary iron on polyunsaturated fatty acid, vitamin E and their derivatives in male rats (Rat에 있어서 탈지사료 및 철분투여가 다불포화 지방산, vitamin E 및 그 유도체에 미치는 영향)

  • Huh, Rhin-sou;Kim, Young-hong;Kim, Sung-hoon;Do, Jae-cheul;Lee, Young-ho;Choi, Yeon-shik
    • Korean Journal of Veterinary Research
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    • v.30 no.4
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    • pp.407-412
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    • 1990
  • This study was designed to elucidate the effects of administration with dietary iron and fat-free diet on the contents of unsaturated fatty acid in phospholipid molecules, vitamin E contents and malondialdehyde contents in liver, kidney, muscle and testis of the male rats. The rats were divided into 3 experimental groups, namely, control, iron injection and fat-free diet administration groups. The control group was fed with normal diet, iron injection group injected intraperitoneally 20mg of ferric hydroxide/100g of body weight 20 times every 3 days and fat-free diet group administered lipid extraction diet with hexane in normal diet. All experimental groups were maintained for 60 days with feeding on the respective ration. The results obtained were summarized as follows: 1. In the mean contents of unsaturated fatty acid in phospholipid of liver, kidney, muscle and testis among groups, control group was 21.31mg/g, 19.38mg/g, 1.67mg/g, 13.68mg/g, iron injection group was 13.83mg/g, 16.53mg/g, 0.71mg/g, 10.11mg/g and fat-free diet group was 21.07mg/g, 19.38mg/g, 1.49mg/g and 13.40mg/g, respectively. 2. In the mean contents of vitamin E in liver, kidney, muscle and testis among groups, control group was 6.77mg/g, 1.93mg/g, 0.12mg/g, 0.17mg/g, iron injection group was 3.16mg/g, 0.86mg/g, 0.07mg/g, 0.09mg/g and fat-free diet group was 7.41mg/g, 1.50mg/g, 0.11mg/g and 0.16mg/g, respectively. 3. In the mean contents of malondialdehyde in liver, kidney, muscle, testis and serum among groups, control group was 11.29nM/0.1g, 23.25nM/0.1g, 42.47nM/0.1g, 7.01nM/0.1g, 4.33nM/ml, iron injection group was 34.98nM/0.1g, 40.55nM/0.1g, 72.21nM/0.1g, 12.26nM/0.1g, 11.27nM/ml and fat-free diet group was 8.07nM/0.1g, 20.63nM/0.1g, 39.92nM/0.1g, 6.95nM/0.1g and 4.27nM/ml, respectively.

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Changes of Some Physicochemical Properties of Yoghurt made from ${\beta}$-Galactosidase-treated Commercial Milks (${\beta}$-Galactosidase 처리 시유로 제조한 요구르트의 이화학적 성분 변화)

  • Lee, In-Seon;Kim, Sang-Hee;Ha, Jae-Ho;Kang, Kook-Hee
    • Korean Journal of Food Science and Technology
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    • v.21 no.6
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    • pp.795-799
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    • 1989
  • This study was carried out to hydrolyze lactose in commercial milk by ${\beta}-galactosidase$ from Kluyveromyces fragilis and to compare some physicochemical properties of yoghurts made from control and lactase-treated commercial milks. Quantitative analysis of sugars was performed by gas liquid chromatograph (GLC) on trimethylsilyl (TMS) derivatives. In commercial milk, 94.6% of lactose was hydrolyzed after 2 hours incubation at $40^{\circ}C$ with 6.0 units/ml of ${\beta}-galactosidase$. pH, titratable acidity and viable cell number of yoghurt made from lactase-hydrolyzed (LH) commercial milk were 4.1, 1.04% and $6.5{\times}10^8/ml$ of Str. thermophilus, $8.9{\times}10^8/ml$ of L. bulgaricus after 8 hours incubation at $40^{\circ}C$, respectively, The total contents of amino acid were 2.63% in control and 2.19%. in LH yoghurt. The total contents of free amino acid were 26.95 mg% in control and 17.55mg% in LH yoghurt. Analysis of free fatty acids resulted in that the contents of short chain fatty acids in LH yoghurt were a little higher than those in control. Both in control and LH yoghurt, the palmitic acid content was highest and that was followed by oleic and myristic acid.

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EFFECT OF EMD ON HUMAN PERIODONTAL LIGAMENT-DERIVED CELLS AND OSTEOBLAST-LIKE CELLS (MC3T3-E1) IN HIGH GLUCOSE CONDITION (고농도 포도당 환경에서 EMD(Enamel Matrix Derivatives)가 인간 치주인대 세포와 뼈모세포양 세포(MC3T3-E1)에 미치는 영향)

  • Lee, Baek-Soo;Kim, Sun-Wook;Jue, Sung-Sook;Kwon, Yong-Dae
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.34 no.5
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    • pp.532-536
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    • 2008
  • Purpose: This study was designed to evaluate effect of EMD on proliferation of HPDLCs and MC3T3-E1 cells in high glucose condition in vitro. Material and method: The Human PDL fibroblasts(HPDLCs) were obtained through typical way and the cells used in this experiment were divided in 4 groups. $1{\times}10^4/ml$ HPDLCs suspension was cultured in typical DMEM and assigned to group 1. The cells cultured in DMEM which included 400mg/dl glucose are allocated to group 3. Group 2 and 4 are established by adding EMD to group 1 and 3 respectively. These control and experimental groups had been cultured for 24 and 48 hours, and MTT assay was conducted. The differences of each group in cellular proliferation was evaluated. The same experiment was conducted for preosteoblast (MC3T3-E1) with adding $25\;{\mu}g/ml$ EMD. Results: EMD had the same effect on both PDL cells and MCT3T3-E1 cells. The experimental group had more meaningful differences and active cellular proliferation than the control group did. The EMD accelerated cellular proliferation not only in normal glucose condition but also in high glucose condition. The same results were observed via MTT assay; EMD-added experimental group had more meaningful differences and showed higher cellular activity than control group did. Each experimental and control group was inspected for statistical significance through Kruskal-Wallis Test. Statistical significances were observed among these groups. (SPSS 12.0 Chicago, IL, USA, p=0.008, p=0.011) Conclusion: EMD is considered to accelerate proliferation of PDL cells and MC3T3-E1 cells in high glucose condition as well as normal glucose condition.