• Title/Summary/Keyword: 2-p-opt

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Synthesis and quantative structure-activity relationships on the antifungal activity of 3-phenylisoxazol and 3-phenyl-2,5-dihydro-5-isoxazolone derivatives (3-phenylisoxazole 및 3-phenyl-2,5-dihydroisoxazol-5-one 유도체의 합성과 살균활성에 관한 구조-활성관계)

  • Sung, Nack-Do;Yu, Seong-Jae;Lee, Hee-Chul
    • The Korean Journal of Pesticide Science
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    • v.5 no.4
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    • pp.20-26
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    • 2001
  • A series of new 2-benzoyl-3-phenyl-2,5-dihydroisoxazol-5-one, (A) and 3-phenyl-5-phenylcarbonyl-oxyisoxazole, (B) derivatives as substrates were synthesized and their quantitative structure-activity relationships (QSAR) analyses between the antifungal activities ($pI_{50}$) and physicochemical parameters of substituents onl the benzoyl group against resistant (RPC:95CC7303) and sensitive (SPC:95CC7105) Phytophthora blight (Phytophthora capsici,) were studied. The synthetic yield (%) and antifungal activities of (A) were higher than (B) and selectivities between the fungi were not showed. From the basis on the Hansch-Fujita analyses, the optimum width values ($(B_2)_{opt.}=ca.\;4.00{\AA}$) of the substituents on the benzoyl group were important factor in determining fungicidal activity against the two fungi. Influence of the substituents as electron withdrawing group on the fungicidal activity against RPC, but not for SPC. And tile bromo- and acetyl-substituents were contributed to higher antifungal activity against RPC and SPC from the results of Free-Wilson analyses.

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Phenyl substituent effect on the fungicidal activity of N-Phenyl-O-phenylthionocarbamate derivatives (N-Phenyl-O-phenylthionocarbamate 유도체의 항균활성에 미치는 phenyl 치환기의 효과)

  • Sung, Nack-Do;Soung, Min-Gyu
    • The Korean Journal of Pesticide Science
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    • v.3 no.1
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    • pp.29-36
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    • 1999
  • A series of N-phenyl-O-phenylthionocarbamate derivatives were synthesized and determinated fungicidal activities in vitro against gray mold (Botrytis cinerea) and capsicum phytophthora blight (Phytophthora capsici) which showed resistance and sensitivity to benomyl and metalaxyl as systemic fungicides, respectively. The structure-activity relationship (SAR) was investigated by Free-Wilson analysis method and Hansch method. From the basis on the findings, the N-phenyl(X) groups had more contributions than O-phenyl(Y) groups did and ortho-substituents on the N-phenyl group showed high fungicidal activities. Especially, 4-cyano substituent, 2 as X-group showed 50% inhibition($pI_{50}=5.50$) of hyphae growth at 0.8ppm against resistance P. capsici (RPC) And hydroxyl substituents, 12 and 23 displayed the highest fungicidal activity against resistant B. cinerea (RBC), sensitive B. cinerea (SBC), and sensitive P. capsici (SPC). Antifungal activities of SPC were dependent upon molar refractivity (MR) constant and those of others relied on hydrophobic parameters (${\sigma}$ and logP). For increasing fungicidal activity against RPC and SBC, the optimum values of the sigma (${\sigma}$) and field(F) constants as electron withdrawing groups were 0.32 and 0.18, respectively.

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Structure-activity relationships on the selective herbicidal activity between rice plant and barnyard grass by the N-phenyl substituents in 2-(4-(6-chloro-2-benzoxazolyloxy)-phenoxy)-N-phenyl propionamide derivatives (2-(4-(6-chloro-2-benzoxazolyloxy) phenoxy)-N-phenyl propionamide 유도체 중 N-phenyl 치환체들에 의한 벼와 피의 선택적 제초활성에 미치는 구조-활성관계)

  • Sung, Nack-Do;Lee, Sang-Ho;Chang, Hae-Sung;Kim, Dae-Whang;Kim, Jin-Suk
    • The Korean Journal of Pesticide Science
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    • v.3 no.3
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    • pp.11-19
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    • 1999
  • A some of synthesized 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenyl propionamide derivativesa substrates were found to selectivity significantly with both rice plant (Oryza sativa L.) and barnyard grass (Echinochloa crus-galli) for those her- bicidal activities with post emergence in up land. The selectivity of substrates against rice plant better than that of Fenoxaprop-ethyl. The structure activity relationship (SAR) n the selectivity of N-phenyl substituents were analyzed by the Free-Wilson and Hansch method. The SAR approach against barnyard grass is shown that the optimal ($({\pi})_{opt.}=1.60$) hydrophobicity and electron donating effects ($0<{\sigma}$ & 0$(ES)_{opt.}=0.87$) so that the herbicidal activity against rice plant can be decreased. The significance of these results on the selectivity between barnyard grass and rice plant is discussed. And it is assumed that the 2-ethoxy-3-methoxy-4-dimethylamino group substituent ($pI_{50}$=6.60, 1g/ha) is selected as the most highest herbicidal activity against barngard grass in green house.

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Influence of substituted phenoxy group on the fungicidal activities of 2-N-benzyl-5-phenoxy-3-isothiazolone derivatives (2-N-benzyl-5-phenoxy-3-isothiazolone 유도체의 살균활성에 미치는 치환-phenoxy기의 영향)

  • Sung, Nack-Do;Kim, Ki-Hyun
    • The Korean Journal of Pesticide Science
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    • v.5 no.3
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    • pp.36-40
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    • 2001
  • A series of new 2-N-benzyl-5-phenoxy-3-isothiazolone derivatives were synthesized and their in vitro antifungal activities against resistant Phytophthora capsici (RPC) & sensitive Phytophthora capsici (SPC) with metalaxyl fungicide have been measured. In addition, influence of substituted 5-phenoxy group on the -antifungal activities ($pI_{50}$) and the reactivity of substrates were investigated. From the results, reactivity of none substituted substrate showed tendency displaying orbital-controlled reaction. The substituents on the 5-phenoxy ring showed selective fungicidal activity between SPC and RPC. Especially, the 4-fluoro substituent, 6 in the RPC and 4-nitro substituent, 3 in SPC exhibited strongly selective antifungal activity among them. The activities on the SPC would depend largely on the optimal molar refractivity ($MR_{(opt.)}=7.37cm^3/mol$) whereas the activities on the RPC would depend largely on the optimal highest occupied molecular orbital energy ($HOMO_{(opt.)}=-9.2137e.v.$) and weak electron donating (${\sigma}<0$) group. And Free-Wilson analyses revealed that the antifungal activity against RPC depends on the methoxy and bromo-substituent and all of the substituents contribute to antifungal activities against SPC.

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Isolation of Bacillus sp. SW29-2 and Its Antifungal Activity against Colletotrichum coccodes (Bacillus sp. SW29-2의 분리 및 Colletotrichum coccodes에 대한 항진균 활성)

  • Han, Yeong-Hwan
    • Journal of Life Science
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    • v.27 no.6
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    • pp.688-693
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    • 2017
  • Antifungal bacterium against Colletotrichum coccodes causing black dot disease of potatoes and anthracnose of tomatoes was isolated from sewage sludge. The isolate showed a 99% sequence homology of partial 16S rRNA of Bacillus methylotrophicus CBMB205 and Bacillus amyloliquefaciens subsp. plantarum FZB42. The isolate was identified as Bacillus sp. SW29-2, using the neighbor-joining phylogenetic tree, BlastN sequence analysis, and morphological and cultural characteristics. Bacillus sp. SW29-2 is an aerobic, Gram-positive, endospore-forming bacterium, of which the morphological and physiological characteristics were the same as those of type strain B. lichniformis CBMB205, except for the cell growth of over 4% NaCl. The cell growth of the temperature and the initial pH of the medium was shown at $18-47^{\circ}C$ (opt. ca. $38^{\circ}C$) and 3-9 (opt. ca. 6.0), respectively. The inhibition size (diameter) of Bacillus sp. SW29-2 against four strains of C. coccodes ranged from 23 to 29 mm. Also, the isolate showed antifungal activity against penicillium rot-causing Penicillium expansum in apples. Thus far, any report on the antifungal activity of Baciilus spp. against C. coccodes has not been found. These results suggest that the Bacillus sp. SW29-2 isolate could be used as a possible biocontrol agent against C. coccodes, and further applied to other plant pathogenic fungi.

The Cytotoxicity of 1,3-diphenylpropenone derivatives (1,3-diphenylpropenone 유도체의 세포독성)

  • Yu, Seong-Jae;Kwon, Byung-Mok;Lee, Chong-Ock;Choi, Sang-Un;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.42 no.1
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    • pp.68-72
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    • 1999
  • The cytotoxicity of 1,3-diphenylpropenone derivatives known to inhibit the farnesyl protein transferase (FPTase) was examined against various established tumor cell line, A549 (lung cancer), SKMEL-2 (uterine cancer), HCT-15 (skin cancer), SKOV-3 (brain cancer) and XF-498 (colon cancer) of the 1,3-diphenylpropenone derivatives showing farnesyl protein transferase (FPTase) inhibition activity. And the structure-activity relationship (SAR) between structure of 1,3-diphenylpropenone derivatives as substrate and cytotoxicity was investigated by Free-Wilson analysis as well as Hansch method with tumor cell lines. From the result of Free-Wilson analyses, X-substituents on the benzoyl group have a more important role than Y-substituents on the styryl group. The 2,4-dichloro substituent, 15 and 2,4-dimethyl substituent, 16 showed the highest cytotoxicity (average pI_(50)=5.0). Particulary, the cytotoxicity of X-substituents increased with electronic effect $({\sigma})$ due to weak electron withdrawing group with optimum value $({\sigma}_{opt}=0.22{\sim}0.29})$ whereas that of Y-substituent resulted from various factors such as logP, $B_1$ and R constant.

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Structure-activity relationships on the herbicidal activity of the 2,3-dihydro-2-ethyl-2,4,6,7-tetramethylbenzofuran-5-yl substituents in 5-benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one derivatives (5-Benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one 유도체 중 2,3-dihydro-2-ethyl-2,4,6,7-tetramethylbenzofuran-5-yl 치환체들의 제초활성에 관한 구조-활성관계)

  • Sung, Nack-Do;Song, Jong-Hwan;Kim, Kyoung-Mahn
    • The Korean Journal of Pesticide Science
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    • v.4 no.3
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    • pp.34-39
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    • 2000
  • A new fifteen 2,3-dihydro-2-ethyl-2,4,6,7-tetramethylbenzofuran-5-yl substituents in 5-benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one derivatives as substrate were synthesized and their herbicidal activities against rice plant (Oryza sativa L.) and barnyard grass (Echinochloa crus-galli) with post emergence were measured under submerged conditions. The $R_{1}$=methyl substituents, $1{\sim}8$ showed the higher herbicidal activity to the rice plant and barnyard grass. The structure-activity relationships (SARs) on tile herbicidal activity of $R_{1}$ and $OR_{2}$ groups on the azomethine bond in substrates were analysized. From tile results of dicussed SAR, the herbicide activities against rice plant would depend largely on the steric factor, Whereas, in case of barnyard grass, the activities were governed by the hydrophobicity factor. The conditions of selective herbicide activity between the two plant species are assumed that the substrates should nave optimal hydrophobicity ( $(logP)_{opt.}=6.0$), a $R_{1}$ groups of small and a long $OR_{2}$ groups.

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Studies on the Proteolytic Enzyme Produced by Rhizopus japonicus S-62 (Rhizopus japonicus S-62가 생성(生成)하는 단백질분해효소(蛋白質分解酵素)에 관(關)한 연구(硏究))

  • Chung, Man-Jae
    • Korean Journal of Food Science and Technology
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    • v.9 no.1
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    • pp.31-35
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    • 1977
  • As a study on the acid protease production by Rhizopus japonicus S-62, the culture conditions for the enzyme production and characteristics of the crude enzyme were investigated. The results are summarized as follows: 1. The optimum conditions for solid culture on wheat bran were 48 hrs of culture period and $100{\sim}120%$ addition of tap water. 2. Of the several media, wheat bran medium was the most excellent in the enzyme production. 3. The addition of sucrose, fructose, $NH_4Cl$ and $NaH_2PO_4$ on wheat bran, respectively, increased largely the enzyme production. 4. The optimum pH for the enzyme action was pH $2.4{\sim}2.6$, the optimum temperature was about $40^{\circ}C$, and the stable pH range was $pH\;2.5{\sim}5.0$, the enzyme was stable below $40^{\circ}C$ and was inactivated abruptly above $40^{\circ}C$.

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Investigation of Annealing Effect for a-SiC:H Thin Films Deposited by Plasma Enhanced Chemical Vapor Deposition (플라즈마 화학기상 증착방식으로 성장시킨 비정질 실리콘 카바이드 박막의 열처리 효과에 관한 특성분석)

  • 박문기;김용탁;최원석;윤대호;홍병유
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.13 no.10
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    • pp.817-821
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    • 2000
  • In this work, we have investigated the dependence of annealing temperature(T$\_$a/) on optical and electrical properties of amorphous hydrogenated SiC(a-SiC:H) films. The a-SiC:H films were deposited on corning glass and p-type Si(100) wafer by PECVD (plasma enhanced vapor deposition) using SiH$_4$+CH$_4$+N$_2$ gas mixture. The experimental results have shown that the optical energy band gap(E$\_$opt/)of the thin films annealed at high temperatures have shown that the graphitization of carbon clusters and micro-crystalline silicon occurs. The current-voltage characteristics have shown good electrical properties at the annealed films.

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The Effect of Active Learning on Critical Thinking Disposition, Problem Solving Ability, and Self-leadership of Nursing Students in Online Nursing Health Assessment Practice Class (온라인 건강사정실습 수업에서 능동학습이 간호대학생의 비판적사고성향, 문제해결능력, 셀프리더십에 미치는 효과)

  • Ma, Hyunhee
    • The Journal of the Convergence on Culture Technology
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    • v.8 no.5
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    • pp.39-50
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    • 2022
  • The Purpose of this study was to confirm the effects of Active learning application on thecritical thinking disposition, problem-solving ability, and self-leadership of nursing students in the online health assessment practice course in the COVID-19 pandemic situation. Data collection was conducted from September 1st to December 17th, 2021 for 78 nursing students in the Department of Nursing at University D, and the collected data was analyzed using the SPSS/WIN 20 program. As a result of this study, the critical thinking disposition (t=-2.11 p=.038) and self-leadership (t=-2.07 p=.042) were statistically significantly increased after active learning was applied to the online nursing health assessment practice class. SOAP, Outcome-Present-Test(OPT) worksheet, clinical reasoning webs, mind map writing are confirm to improve critical thinking disposition, problem solving ability, self-leadership of nursing student, so research to confirm the effect in face to face classed should be conducted.