• 한국응용과학기술학회지
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• 제14권2호
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• pp.93-102
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• 1997

Isothiazoline derivatives is widely used to food, medical drug and industrial goods, cosmetics etcs, and it makes to restrain and to sterilize a breeding of microbe as a preservative and a sterilizing agent. It differs with the raw material of paraoxybenzoic acid derivatives or imidazolydinyl urea to be in use at present, on the efficacy and effect, and has various characteristics. This synthesis makes 3,3'-dithiodipropionic chloride to add a thionyl chloride in 3,3'-dithiodipropionic acid, and 3,3'-dithiodipropionic methyl amide makes to synthesize in a reflux reaction the mono methyl amine to 3,3'-dithiodipropionic chloride. And last synthesis becomes to make chlorination-cyclization molecule doing a reflux reaction in the temperature of $90{\sim}100^{\circ}C$ to mix excessively thionyl chloride and ethylene dichloride to 3,3'-dithiodipropionic methyl amide. The last synthesis material has got in the mixture of 5-chloro-2-methyl-4-isothiazoline-3-one and 2-methyl-4-isothiazoline-3-one, and it is so-called isothiazoline derivatives. The purification of isothiazoline derivatives makes to fuse in ethyl acetate, and makes to decolorize and to deodorize in recrystallization. This experiment has been in synthesis and purification of isothiazoline derivatives, and has tried to measure on the antisepsis and sterilization function of microbe according to pH or content change.

• Asian-Australasian Journal of Animal Sciences
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• 제19권9호
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• pp.1305-1313
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• 2006

Five male dairy goats (Saanen), 4.6 month old with a body weight of 21.4 ($SD{\pm}1.6$) kg, were used to examine 5 dietary urea treatments in a $5{\times}5$ Latin Square experimental design. The five levels of urea were 10, 20, 30, 40 and 50 g urea/kg DM of steam-treated oil palm fronds (OPF) and dry matter intake tended (p>0.05) to increase with increasing urea supplementation up to 30 g/kg OPF (77.7 g/kg $BW^{0.75}$), but decreased (p<0.05) with 40 and 50 g urea/kg OPF (67.4 and 63.7 g/kg BW0.75, respectively) supplementation. Similarly, dry matter, organic matter, crude protein, neutral detergent fiber and hemicellulose digestibilities increased (p<0.05) with the addition of urea to 30 g/kg OPF but thereafter decreased (p<0.05) with 40 and 50 g/kg OPF. Ruminal pH, ruminal $NH_3$-N concentration and plasma urea concentration increased linearly (p<0.01) and quadratically (p<0.01) as a consequence of addition of urea to the diet. Excretion of total purine derivatives (PD) by goats fed 30 g of urea/kg OPF was highest (p<0.05) followed by goats fed 20, 40, 10 and 50 g of urea/kg OPF. Microbial N (g N/day) and efficiency of microbial N supply expressed as g N/kg organic matter apparently digested in the rumen were higher (p<0.05) in goats fed 30 g of urea/kg OPF (5.5 g N/day and 22.0 g N/kg DOMR, respectively) than in goats on 10 and 50 g of urea/kg OPF treatments. However, the former did not differ from goats fed 20 g of urea/kg OPF (3.9 g N/day and 16.6 g N/kg DMOR, respectively). Ruminal VFA concentration, protein/energy ratio, N absorption and N retention increased (p<0.05) with the addition of urea to the diet up to 30 g/kg OPF but decreased (p<0.05) with 40 and 50 g/kg OPF. This implies that the optimal level of urea supplementation in an OPF based diet was about 30 g urea/kg OPF.

• Bulletin of the Korean Chemical Society
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• 제32권3호
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• pp.1091-1094
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• 2011

• Environmental Analysis Health and Toxicology
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• 제15권1_2호
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• pp.53-59
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• 2000

The purpose of this study is the development of the simple and precise determination method of ethyl isocyanate (EIC) and propyl isocyanate (PIC) through derivatization using secondary aliphatic amines by gas chromatography with flame ionization detector. The urea derivatives are quantitatively and simultaneously derived from EIC and PIC with secondary aliphatic amines such as dipropylamine, dibutylamine. and dipentylamine in methylene chloride, and confirmed by thin layer chromatography and gas chromatography with mass selective detector. For GC/FID, according to the increasing carbon atom of the amines, the retention time and peak area of the urea derivatives are increased. The instrumental detection limits for EIC and PIC were about 23.3∼34.8 $\mu\textrm{g}$ and 21.6∼28.9 $\mu\textrm{g}$, respectively.

• 통합자연과학논문집
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• 제10권3호
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• pp.141-147
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• 2017

Vascular endothelial growth factor (VEGF) is an important signaling protein involved in angiogenesis, which is the formation of new blood vessels from pre-existing vessels. Consequently, blocking of the vascular endothelial growth factor receptor (VEGFR-2) by small molecule inhibitors leads to the inhibition of cancer induced angiogenesis. In this study, we performed a two dimensional quantitative structure activity relationship (2D-QSAR) study of 38 N-Phenyl-N'-{4-(4-quinolyloxy) phenyl} urea derivatives as VEGFR-2 inhibitors based on hologram quantitative structure-activity (HQSAR). The model developed showed reasonable $q^2=0.521$ and $r^2=0.932$ values indicating good predictive ability and reliability. The atomic contribution map analysis of most active compound (compound 7) indicates that hydrogen and oxygen atoms in the side chain of ring A and oxygen atom in side chain of ring C contributes positively to the activity of the compounds. The HQSAR model developed and the atomic contribution map can serve as a guideline in designing new compounds for VEGFR-2 inhibition.

• Archives of Pharmacal Research
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• 제27권9호
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• pp.885-892
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• 2004

Due to the rapidly growing number of resistant strains of bacteria, the search for antibacterial agents with new modes of action will always remain an important and challenging task. Thus, the reaction of 2-substituted or. unsubstituted-4-(4-acetylanilino)-5,6,7,8-terahydrobenzo［b］ thieno［2,3-d］pyrimidine derivatives 1-3 with the hydrazine derivatives, semi and / or thiosemi-carbazides, provided the corresponding hydrazones 4-6 and semi and/or thiosemicarbazones 7-9. Claisen-Schmidt condensation of compounds 1 or 2 with the appropriate aldehyde yielded the chalcones 10, 11 which, when treated with hydroxylamine hydrochloride gave rise to the isoxazoline-containing compounds 12, 13. Furthermore, reacting the respective chalcones 10, 11 with different hydrazines, urea and/or thiourea, furnished compounds 14, 15, 16, and 17 respectively. Representative compounds were tested for their antimicrobial activity against Candida Albicans and certain gram-positive and gram-negative bacteria. Their MICs were then determined. Compound 15e, showed a broad spectrum of activity while most of the other com-pounds showed varying antimicrobial activity.

• Asian-Australasian Journal of Animal Sciences
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• 제27권5호
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• pp.658-666
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• 2014

This study aimed to evaluate urea excretion, nitrogen balance and microbial protein synthesis in lactating goats fed with diets containing different protein sources in the concentrate (soybean meal, cottonseed meal, aerial part of cassava hay and leucaena hay). Four Alpine goats whose mean body weight was $42.6{\pm}6.1kg$ at the beginning of the experiment, a mean lactation period of $94.0{\pm}9.0days$ and a production of $1.7{\pm}0.4kg$ of milk were distributed in a $4{\times}4$ Latin square with four periods of 15 days. Diets were formulated to be isonitrogenous, containing 103.0 g/kg of CP, 400 g/kg of Tifton 85 hay and 600 g/kg of concentrate. Diet containing cottonseed meal provided (p<0.05) increased excretion of urea and urea nitrogen in the urine (g/d and mg/kg of BW) when compared with leucaena hay. The diets affected the concentrations of urea nitrogen in plasma (p<0.05) and excretion of urea nitrogen in milk, being that soybean meal and cottonseed meal showed (p<0.05) higher than the average aerial part of the cassava hay. The use of diets with cottonseed meal as protein source in the concentrate in feeding of lactating goats provides greater nitrogen excretion in urine and negative nitrogen balance, while the concentrate with leucaena hay as a source of protein, provides greater ruminal microbial protein synthesis.

• Asian-Australasian Journal of Animal Sciences
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• 제15권7호
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• pp.992-997
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• 2002

Two in vivo experiments were conducted to evaluate the effect of novel urease inhibitor hydroquinone (HQ) on ammonia release rate from urea hydrolysis, nitrogen balance, nutrient digestibility and efficiency of microbial protein synthesis. In Exp. 1, twelve crossbred cannulated lambs were randomly assigned within initial body weight block to one of four HQ treatments, which included 0 (control), 30, 60 or 80 mg HQ/kg DM intake. Ammonia concentration and pH of ruminal fluid were immediately measured at 0, 2, 4, 6 and 8 h after feeding. Increasing the dose of HQ tended (p<0.15) to linearly decrease NH3 formation. The ammonia peak concentration (2 h post-feeding) in animals receiving HQ was approximately one-half of that in animals not receiving HQ (p<0.01), and a relatively sustained ammonia release could be obtained at the dose of 30 or 60 mg HQ/kg DM. In Exp. 2, sixteen intact crossbred lambs (weight $40{\pm}0.8kg$) were used in a $2{\times}2$ factorial design experiment. The four rations consisting of soybean meal-based (SBM) or urea-based (Urea) nitrogen source with or without HQ (S1, S0, U1 and U0) were fed in digestion and N balance trials. Apparent digestibility of major nutrients except that of ADF was not affected by either nitrogen source or addition of HQ. Regardless of nitrogen source, supplementation of HQ significantly improved ADF digestibility (p<0.05). The various ration had no effects on N metabolism in the presence of HQ. There was significant difference between total purine derivatives (PD), estimated efficiency of microbial N synthesis (p<0.05) and urea-N excretion (p<0.01) in the urine for the SBM ration and for the Urea ration. However, HQ had little influence on efficiency of microbial N synthesis as proportion of daily intake of total tract digestible OM (p>0.05). No interactions between main nitrogen source and HQ were measured throughout the trial. Results of this study suggest that addition of HQ to ration may improve ADF digestion with having no negative effect on N metabolism and microbial protein production.

• Asian-Australasian Journal of Animal Sciences
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• 제11권6호
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• pp.661-672
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• 1998

Two experiments were conducted to examine the effects of a range of concentrations of ruminal fluid ammonia ($NH_3$-N) on forage digestibility, microbial growth efficiency and the mix of microbial species. Urea was either continuously infused directly into the rumen of sheep fed 33.3 glh of oaten chaff (Exp. I) or sprayed onto the oaten chaff (750 g/d) given once daily (Exp. 2). Concentrations of $NH_3$-N increased with incremental addition of urea (p < 0.01). Volatile fatty acids (VFA) concentrations and 24 h in sacco organic matter digestibility in the rumen were higher when supplemental urea was given (p < 0.01). The (C2 + C4) : C3 VFA ratio was lower (p < 0.05) when $NH_3$-N was above 200 mgN/I. The fungal sporangia appearing on oat leaf blades were significantly higher when urea was supplemented, indicating that $NH_3$-N was a growthlimiting nutrient for fungi at levels of $NH_3$-N below 30 mgN/l. The density of protozoa was highest when $NH_3$-N concentrations were adjusted to 30 mgN/I for continuously fed ($4.4{\times}10^5/ml$) and to 168 mgN/1 for once daily feeding ($2.9{\times}10^5/ml$). Thereafter increasing concentrations of $NH_3$-N, were associated with a concomitant decline in protozoal densities. At the concentration of $NH_3$-N above 200 mgN/l, the density of protozoa was similar to the density of protozoa in ruminal fluid of the control sheep ($1.8{\times}10^5/ml$). The efficiency of net microbial protein synthesis in the rumen calculated from purine excretion was 17-47% higher when the level of $NH_3$-N was above 200 mgN/1. The possibilities are that 1) there is less bacterial cell lysis in the rumen because of the concomitant decrease in the protozoal pool and/or 2) microbial growth per se in the rumen is more efficient with increasing $NH_3$-N concentrations.

• 약학회지
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• 제51권4호
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• pp.246-252
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• 2007

Several ureas and thioureas were designed and synthesized and their inhibitory activities of NO production in lipopolysaccharide-activated macrophages were evaluated. Among these compounds, indole-containing thiourea 6e was the most potent showing 17.4 ${\mu}M$ of $IC_{50}$ value.