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Synthesis and antifungal activities of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl]piperidine derivatives on Phytophthora capsici (4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl] piperidine 유도체들의 합성과 고추역병균에 대한 살균활성)

  • Nam, Seok-Woo;Lee, Gyung-Rak;Kim, Tae-Joon;Chung, Bong-Jin;Choi, Won-Sik
    • The Korean Journal of Pesticide Science
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    • v.16 no.1
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    • pp.1-10
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    • 2012
  • Fungicidal activities against phytopathogenic fungi of diarylthiazole compound of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (I) have been determined to be excellent and compound I was used as the leading compounds in this study. Furthermore, the compound was synthesized by reacting them with five functional groups, 4-fluoro-3-methylphenyl, 4-fluoro-3-chlorophenyl, 4-chloro-2-fluorophenyl, 4-bromo-3-methylphenyl and 2,4-dichlorophenyl groups instead of 4-fluorophenyl group. Also, 2-amino-, 2-(N-ethoxycarbonyl)piperidin-4-yl-, and 2-piperidin-4-yl-thiazole were introduced as the leads instead of 2-N-methylpiperidine-4-yl-thiazol of compound I. VIII-1~VIII-5 and XIII-1~XV-5 compounds were newly synthesized and their structures were confirmed by $^1H$-NMR-spectrum. The fungicidal activities of all the synthesized compounds against Phytophthora capsici were examined using the whole plant method. Among the VIII-1~VIII-5 and XIII-1~XV-5 chemicals, XIV-3 showed the most potent antifungal activity in vivo. While the $EC_{50}$ and $EC_{90}$ values of the commercial fungicide dimethomorph and I were $4.26{\pm}0.02$, $14.72{\pm}0.05$ and $1.01{\pm}0.11$, $6.31{\pm}0.09mM$, those of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-chloro-2-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (XIV-3) was $0.98{\pm}0.21$ and $5.85{\pm}0.05mM$. Therefore, XIV-3 can be considered as a viable candidate for the control of plant diseases caused by P. capsici, and further studies will be conducted on the mode of action XIV-3.

Analysis of Systemic Pesticide Imidacloprid and Its Metabolites in Pepper using QuEChERS and LC-MS/MS (QuEChERS 전처리와 LC-MS/MS를 이용한 고추 중 침투성농약 Imidacloprid 및 대사물질 동시분석법)

  • Seo, Eun-Kyung;Kim, Taek-Kyum;Hong, Su-Myeong;Kwon, Hye-Yong;Kwon, Ji-Hyung;Son, Kyung-Ae;Kim, Jang-Eok;Kim, Doo-Ho
    • The Korean Journal of Pesticide Science
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    • v.17 no.4
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    • pp.264-270
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    • 2013
  • Imidacloprid is a systemic insecticide which act as an insect neurotoxin. It used for control of pest such as aphids and other sucking insects in fruits and vegetables. Systemic pesticides move inside a crop following absorption by the plant, and these were converted into a variety of metabolites. Sometimes these metabolites make a problem about safety of agricultural products. So a simultaneous determination method of pesticide and its metabolites is needed, to monitor their presence in agricultural product and study on the fate of pesticide in a plant. This study's aim is to investigate simultaneous analysis method of imidacloprid and its metabolites, imidacloprid guanidine, imidacloprid olefin, imidacloprid urea, and 6-chloronicotinic acid in red pepper using QuEChERS method and LC-MS/MS systems. QuEChERS method was modifed beacuase $MgSO_4$ salts decreased the recoveries of 6-chloronicotinic acid in extraction procedure. Imidacloprid and its metabolites were extracted by acetonitrile with 1% glacial acetic acid and the extracts were purified through QuEChERS with primary secondary amine (PSA) and $C_{18}$ and analyzed with LC-MS/MS in ESI positive mode. Standard calibration curves were made by matrix matched standards and their correlation coefficients were higher than 0.999. Recovery studies were carried out on spiked pepper blank sample at four concentration levels (0.01, 0.04 and 0.1, 0.4 mg/kg). The average recoveries of imidacloprid and its metabolites were in the range of 70~120% with < 20% RSD. This result indicated that the method using QuEChERS and LC-MS/MS was suitable for the simultaneous determination of imidacloprid and its metabolites in red pepper.

Comparison of Average Glandular Dose in Screen-Film and Digital Mammography Using Breast Tissue-Equivalent Phantom (유방조직등가 팬텀을 이용한 Screen-Film과 Digital Mammography에서의 평균 유선선량)

  • Shin, Gwi-Soon;Kim, Jung-Min;Kim, You-Hyun;Choi, Jong-Hak;Kim, Chang-Kyun
    • Journal of radiological science and technology
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    • v.30 no.1
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    • pp.13-23
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    • 2007
  • In recent years, mammography system is changed rapidly from conventional screen-film system to digital system for application to screening and diagnosis. Digital mammography system provides several advantages over screen-film mammography system. According to the information provided by the manufacturer, digital mammography system offers radiation dose reduction in comparison with screen-film mammography system, because of digital detector, particularly direct digital detector has higher x-ray absorption efficiency than screen-film combination or imaging plate(IP). We measured average glandular doses(AGD) in screen-film mammography(SFM) system with slow screen-film combination, computed mammography(CM) system, indirect digital mammography(IDM) system and direct digital mammography(DDM) system using brest tissue-equivalent phantom(glandularity 30%, 50% and 70%). The results were shown as follows : AGD values for DDM system were highest than those for other systems. Although automatic exposure control(AEC) mode was selected, the curve of the AGD values against thickness or glandularity increased significantly for the SFM system with the uniform target/filter(Mo/Mo) combination. Therefore, the AGD values for the high energy examinations were highest in the SFM system, and those for the low energy examinations were highest in the DDM system. But the curve of the AGD values against thickness and glandularity increased gently for CM system with the automatic selection of the target/filter combination (from Mo/Mo to Mo/Rh or from Mo/Rh to Rh/Rh), and the AGD values were lowest. Consequently, the parameters in mammography for each exposure besides detection efficiency play an important role in oder to estimate a patient radiation dose.

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Effects of Sinetrol-XPur on Leptin-Deficient Obese Mice and Activation of cAMP-Dependent UCP-2 (Leptin 유전자 결핍 동물모델을 이용한 시네트롤(Sinetrol-XPur)의 항비만 효과와 cAMP를 통한 UCP-2 활성화 기전 연구)

  • Yoo, Jae Myeong;Lee, Minhee;Kwon, Han Ol;Choi, Sei Gyu;Bae, Mun Hyoung;Kim, Ok-Kyung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.4
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    • pp.484-491
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    • 2016
  • The present study investigated the effect of Sinetrol-XPur (polyphenolic Citrus spp. and Paullinia cupana Kunth dry extract) and defined the action mode for cyclic adenosine monophosphate (cAMP)-dependent uncoupling protein (UCP)-2 activation. Leptin-deficient obese mice were treated with two different doses, 100 mg/kg body weight (BW) and 300 mg/kg BW of each AIN93G supplement, for 7 weeks. Treatment of obese mice with both low and high doses of Sinetrol-XPur significantly reduced body weight gain compared to control obese mice. White adipose tissue weight of mice was reduced by 30.96% in high dose-supplemented groups. Serum total cholesterol and triglyceride were reduced by a high dose of Sinetrol-XPur by 20.02% and 30.96%, respectively. Serum level of high density lipoprotein (HDL) was significantly increased by treatment with both doses, as the ratio of HDL to low density lipoprotein increased by 138.78% and 171.49%, respectively. Regarding expression of biochemical factors related to lipid metabolism, fatty acid synthase significantly decreased and UCP-2 increased upon treatment with a high dose of Sinetrol-XPur, but there was no significant difference in lipoprotein lipase and hormone-sensitive lipase. To define cellular mechanism, intracellular cAMP levels in 3T3-L1 adipocytes significantly increased in a dose-dependent manner over the range of $50{\sim}250{\mu}m/mL$. The phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine clearly blocked cAMP, suggesting that Sinetrol-XPur promotes lipolysis of adipocytes through inhibition of cAMP-dependent PDE, resulting in induction of cAMP response element binding protein and UCP-2. These results suggest that Sinetrol-XPur supplementation is a viable option for reducing body weight and fat by improving serum lipid profiles and genetic expression of lipid metabolic factors, especially activation of cAMP-dependent UCP-2.

Study on the Biosynthetic Characteristics of Photosynthetic Pigments in Dodder(Cuscuta australis R. Br.) Plant (실새삼의 광합성색소 생합성특성에 관한 연구)

  • Kim, J.S.;Kwak, H.H.;Kim, B.C.;Cho, K.Y.
    • Korean Journal of Weed Science
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    • v.17 no.3
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    • pp.314-324
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    • 1997
  • This study was conducted to investigate whether 1) photosynthetic pigments(chlorophylls and carotenoids) are formed in dodder plant(Cuscuta australis), 2) there are any characteristics in the pigment biosynthesis, compared to that of other normal plants, and 3) dodder responds to some herbicides having target site on chloroplast. 1. Chlorophyll content of dodder tendrill grown under a natural daylight was 9 times and 50 times lower than that of field bindweed stem and leaf, respectively. 2. The photosynthetic pigment contents varied in different tissues, being higher in a apical region than in a lower region of seedling or tendrill. Chlorophyll wasn't almost observed below the 4th internode from the upper. 3. Pigment contents were greatly dependent on light intensity so that there were 4 to 6 times difference among light conditions. When the shoot containning low pigment contents under natural light, was incubated in growth chamber with various light intensities, the pigment contents were increased by 3 times of initial contents at about 97${\mu}E$ $m^{-2}s^{-1}$PAR. While the change in pigment contents was not observed at above 450${\mu}E$ $m^{-2}s^{-1}$PAR 4. Exogenous supply of 5mM 5-aminolevulinic acid increased protochlorophyllide by 7 times and 1.4 times in the etiolated shoot from field bindweed rhizome and in dodder stem, respectively, showing that dodder relatively has a low response to 5-aminolevulinic acid. 5. Pigment loss was observed in the treatment of paraquat, norflurazon, oxyfluorfen and diuron, and protoporphyrin IX was accumulated by oxyfluorfen as in normal plants Based on above results, several chracteristics of pigment biosynthesis in dodder seem to be summerized as follows. Photosynthetic pigment biosynthesis in Cuscuta australis runs even in low level. The pigment contents is differentially distributed in different regions and their contents seem significantly to be controlled by light intensities. Especially, chloroplast rapidly tends to degenerate with the development of tissue. Some herbicides having target site on chloroplast induce damage to dodder stem but are unlikely to control it well in field, except paraquat, due to low chloroplast activity and parasitic mode of nutrition.

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Outcome of Continuous Renal Replacement Therapy in Children (소아에서 지속적 신대체요법의 치료 결과)

  • LIm, Yeon Jung;Jin, Hyun-seung;Hahn, Hyewon;Oh, Sei Ho;Park, Seong Jong;Park, Young Seo
    • Clinical and Experimental Pediatrics
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    • v.48 no.1
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    • pp.68-74
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    • 2005
  • Purpose : There is growing use of continuous renal replacement therapy(CRRT) for pediatric patients, but reports about the use and outcome of CRRT in children is rare in Korea. We report our experiences of CRRT in critically ill pediatric patients. Methods : We reviewed the medical records of 23 pediatric patients who underwent CRRT at Asan Medical Center between May 2001 and May 2004. We evaluated underlying diseases, clinical features, treatment courses, CRRT modalities and outcomes. Results : Ages ranged from three days to 16 years with a median of five years. Patients weighed 2.4 to 63.9 kg(median 23.0 kg; 10 patients ${\leq}20kg$). The underlying diseases were malignancy(nine cases), multiple organ dysfunction syndrome(five cases), hyperammonemia(four cases), acute renal failure associated with liver failure(three cases), dilated cardiomyopathy(one case) and congenital nephrotic syndrome(one case). Pediatric Risk of Mortality(PRISM) III score was $17.6{\pm}7.6$ and the mean number of failing organs was $3.0{\pm}1.7$. Duration of CRRT was one to 27 days(median : nine days). Eleven patients(47.8%) survived. Chronic renal failure developed in two cases, intracranial hemorrhage in one case, and chylothorax in one case among the survivors. PRISM III score and the number of vasopressor before the start of CRRT was significantly lower in the survivors($12.7{\pm}4.2$ and $0.9{\pm}1.1$) compared with nonsurvivors($22.1{\pm}7.8$ and $2.4{\pm}1.4$)(P<0.05). Conclusion : CRRT driven in venovenous mode is an effective and safe method of renal support for critically-ill infants and children to control fluid balance and metabolic derangement. Survival is affected by PRISM III score and the number of vasopressors at the initiation of CRRT.

Changes of Glutamate and Polyamine Levels of Hippocampal Microdialysates in Response to Occlusion of Both Carotid Arteries in Mongolian Gerbils (뇌허혈 손상에 있어서 해마-세포외액내 Glutamate와 Polyamine 농도의 변동에 관한 연구)

  • Shin, Kyung-Ho;Kim, Hyung-Gun;Choi, Sang-Hyun;Cho, So-Hyun;Chun, Yeon-Sook;Chun, Boe-Gwun
    • The Korean Journal of Pharmacology
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    • v.30 no.3
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    • pp.273-289
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    • 1994
  • Reversible brain ischemia was produced by occluding both common carotid arteries for 5 min, and the effects of aminoguanidine (AG), $DL-{\alpha}-difluoromethylornithine$ (DFMO), MK-801, and nimodipine (NM) on the ischemia induced changes of the polyamine, glutamate and acetylcholine levels in the hippocampus CA1 subfield and the specific $[^3H]\;MK-801$ binding to the hippocampus synaptosomal membranes were studied with a histological reference of the cresyl violet stained hippocampus. The basal putrescine level $(PT:\;74.4{\pm}8.8\;nM)$ showed a rapid increase (up to 1.7 fold) for 5 min of ischemia, remained significantly increased for 6 h, and then resumed the further increase to amount gradually up to about 3 fold 96 h after recirculation. However, the level of spermidine was little changed, and the spermine level showed a transient increase during ischemia followed by a sustained decrease to about 40% of the preischemic level after recirculation. The increase of PT level induced by brain ischemia was enhanced with AG or MK-801, but it was reduced by DFMO or NM. The basal glutamate level $(GT:\;0.90{\pm}0.l4\;{\mu}M)$ rapidly increased to a peak level of $8.19{\pm}1.14\;{\mu}M$ within 5 min after onset of the ischemia and then decreased to the preischemic level in about 25 min after recirculation. And NM reduced the ischemia induced increase of GT level by about 25%, but AG, DFMO and MK-801 did not affect the GT increase. The basal acetylcholine level $(ACh:\;118.0{\pm}10.5\;{\mu}M)$ did little change during/after brain ischemia and was little affected by AG or NM. But DFMO and MK-801, respectively, produced the moderate decrease of ACh level. The specific $[^3H]\;MK-801$ binding to the hippocampus synaptosomal membrane was little affected by brain ischemia for 5 min. The control value (78.9 fmole/mg protein) was moderately decreased by AG and MK-801, respectively but was little changed by DFMO or NM. The microscopic findings of the brains extirpated on day 7 after ischemia showed severe neuronal damage of the hippocampus, particularly CA1 subfield. NM and AG moderately attenuated the delayed neuronal damage, and DFMO, on the contrary, aggravated the ischemia induced damage. However, MK-801 did not protect the hippocampus from ischemic damage. These results suggest that unlike to the mode of anti-ischemic action of NM, AG might protect the hippocampus from ischemic injury as being negatively regulatory on the N-methyl-D-aspartate (NMDA) receptor function in the hippocampus.

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Herbicidal Activities of Dinitroaniline Compounds in Turfgrass (Dinitroaniline계(系) 제초제(除草劑)의 잔디밭에서의 작용특성(作用特性))

  • Lee, Y.D.;Kim, S.J.;Kim, K.W.;Kim, K.U.
    • Korean Journal of Weed Science
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    • v.14 no.4
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    • pp.265-271
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    • 1994
  • This study was conducted to determine the herbicidal activity, persistance, downward movement and effect on bentgrass of 7 dinitroaniline herbicides such as benefin [N-butyl-N-ethyl-2,6-dinitro-4-(trifluoromethyl) benzenamine], beslogine [N,N-dibutyl-2,6-dinitro-4-trifluoromethylaniline], prodiamine [2,4-dinitro-$N^3$,$N^3$-dipropyl-6-(trifluoromethyl)-1,3-benzenediamine], pendimethalin [N-(1-ethylpropyl)-3,4-dimethyl-2,6-dinitrobenzenamine], trifluralin [2,6-dinitro-N,N-dipropyl-4-(trifluoromethyl) benzenamine], ethalfluralin [N-ethyl-N-(2-methyl-2-propenyl)-2,6-dinitro-4-(trifluoromethyl) benzenamine], and oryzalin [4-(diprop-ylamino)-3,5-dinitrobenzene-sulfonamide) together with bensulide [O,O-bis(1-methylethyl) S-[2-[(phenyl-sulfonyl) amino]ethyl]phosphorodithioate] and siduron [N-(2-methylcyclohexyl)-N'-phenylurea) as the control. In addition, distribution of pendimethalin and benefin into bentgrass was also determined. Prodiamine, benefin, and pendimethalin at the 1/16 dose of the recommended rate showed very high herbicidal activity($LD_{90}$) on Digitaria sanguinalis, but ethalfluralin and bensulide showed $LD_{90}$ at the 1/4 dose of the recommended rate, showing difference in herbicidal activities among dinitroaniline herbicides. All the herbicides except for pendimethalin had the lower herbicidal activity in sandy soil than that of clay-loam soil. Benefin, beslogine, prodiamine, oryzalin, bensulide and siduron persisted in the soil for about 50 days, but pendimethalin persisted in the soil for about 35 days, and trifluralin and ethalfluralin for about 25 days. Ethalfluralin, oryzalin and bensulide were the most mobile(downward movement) of the 9 herbicides studied. Less mobility was observed in the turfgrass condition than that of the bare soil. Beslogine bensulide prodiamine and benefin had no injury effect on bentgrass(Agrastis atolonifera L., penncross creeping bent grass). However, herbicides like oryzalin, trifluralin and pendimethalin reduced the dry weight of bentgrass by 12%, 30% and 40%, respectively. No significant difference in distribution of pendimethalin and benefin into inner part of leaves, surface and wax layer of bentgrass was observed, and thus it seems that different phytotoxic effect between pendimethalin and benefin may be attributed to different metabolism and mode of action.

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Occurrence Characteristics of Weed Flora by Regions and Agro-Climatic Zonal in Paddy Fields of Korea (우리나라 지역별 및 농업기후지대별 논잡초 발생상황)

  • Lee, In-Yong;Oh, Young-Ju;Park, Jungsoo;Choi, Jun-Keun;Kim, Eun Jeong;Park, Kee Woong;Cho, Seng-Hyun;Kwon, Oh-Do;Im, Il-Bin;Kim, Sang-Kuk;Seong, Deok-Gyeong;Kim, Chang-Seog;Lee, Jeongran;Seo, Hyun-A;Kim, Whan-Su
    • Weed & Turfgrass Science
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    • v.6 no.1
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    • pp.11-20
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    • 2017
  • Ninety species belonging to 28 families of weeds were identified in Korean rice fields. They were divided by eight provinces and 19 agro-climatic zones to be used as basic data of weed control. Looking at the regional weed occurrence, there were 52 species of 20 families in Gyeonggi, 37 species of 17 families in Gangwon, 41 species of 15 families in Chungbuk, 21 species of 12 families in Chungnam, 24 species of 13 families in Jeonbuk, 54 species of 21 families in Chonnam, 36 species of 20 families in Gyeongbuk, and 32 species of 16 families in Gyeongnam province, respectively. The most dominant family was Poaceae followed by Cyperaceae and Asteraceae. Mostly dominant species were Echinochloa spp., Monochoria vaginalis var. plantaginea, Scirpus juncoides var. hotarui, Eleocharis kuroguwai, and Sagittaria sagittifolia subsp. leucopetala with slight differences among the provinces. Although there were some differences in 18 climate zones from Taebaek sub-highlands to the southern part of the East Coast (except for the Taebaek Highland), the dominant species were Echinochloa spp., Monochoria vaginalis var. plantaginea and Scirpus juncoides var. hotarui. The most dominant family was Cyperaceae followed by Poaceae and Asteraceae. The differences of weed occurrence between provinces and agro-climatic zones were largely influenced by various weather conditions rather than the provinces. The changes in cultivation mode and herbicide use might influence as well.

Developing a Dental Unit Waterline Model Using General Laboratory Equipments (실험실 일반 장비를 이용한 치과용 유니트 수관 모델 개발)

  • Yoon, Hye Young;Lee, Si Young
    • Journal of dental hygiene science
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    • v.16 no.4
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    • pp.284-292
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    • 2016
  • Water supplied through dental unit waterlines (DUWLs) has been shown to contain high number of bacteria. To reduce the contamination of DUWLs, it is essential to develop effective disinfectants. It is, however, difficulty to obtain proper DUWL samples for studies. The purpose of this study was to establish a simple laboratory model for reproducing DUWL biofilms. The bacteria obtained from DUWLs were cultured in R2A liquid medium for 10 days, and then stored at $-70^{\circ}C$. This stock was inoculated into R2A liquid medium and incubated in batch mode. After 5 days of culturing, it was inoculated into the biofilm formation model developed in this study. Our biofilm formation model comprised of a beaker containing R2A liquid medium and five glass rods attached to DUWL polyurethane tubing. Biofilm was allowed to form on the stir plate and the medium was replaced every 2 days. After 4 days of biofilm formation in the laboratory model, biofilm thickness, morphological characteristics and distribution of the composing bacteria were examined by confocal laser microscopy and scanning electron microscopy. The mean of biofilm accumulation was $4.68{\times}10^4$ colony forming unit/$cm^2$ and its thickness was $10{\sim}14{\mu}m$. In our laboratory model, thick bacterial lumps were observed in some parts of the tubing. To test the suitability of this biofilm model system, the effectiveness of disinfectants such as sodium hypochlorite, hydrogen peroxide, and chlorhexidine, was examined by their application to the biofilm formed in our model. Lower concentrations of disinfectants were less effective in reducing the count of bacteria constituting the biofilm. These results showed that our DUWL biofilm laboratory model was appropriate for comparison of disinfectant effects. Our laboratory model is expected to be useful for various other purposes in further studies.