• Title/Summary/Keyword: 4-Amino-2

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Synthetic Studies on Fused Nitrogen-heterocycles from N-Amino-N,N $^\prime$-dihydrodiazinediones (I). Condensation of N-Amino-N,N $^\prime$-dihydrodiazinediones with 1,3-Dicarbonyl Compounds

  • Shin, Sung-Chul;Lee, Youn-Young
    • Bulletin of the Korean Chemical Society
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    • v.9 no.6
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    • pp.359-362
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    • 1988
  • The condensation of 1-amino-1,2-dihydro-3,6-pyridazinedione (1) and 2-amino-2,3-dihydro-1,4-phthalazinedione (2) with 1,3-diketones or 1,3-dialdehydes in polyphosphoric acid gave 6,9-dihydro-6,9-dioxopyridazino [1,2-a][1,2,3]triazines (3-6) and 6,11-dihydro-6,11-dioxo[1,2,3]triazino[1,2-b]phtha lazines (7-10), respectively. The condensation of 2 with 2,4-pentanedione in acetic acid gave N-alkylidene intermediate (11), which was cyclized to 9 by treatment with polyphosphoric acid.

Studies on the Synthesis of Pterdine Substituted Pyridonecarboxylic Acids as Potential Antibacterial Agents and their Antimicrobial Activities (항균제로서 Pteridine이 치환된 Pyridonecarboxylic Acids의 합성 및 항균 작용에 관한 연구)

  • Ryu, Seoung Ryuall;Choo, Dong Joon
    • Applied Chemistry for Engineering
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    • v.7 no.6
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    • pp.1096-1104
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    • 1996
  • In order to synthesize a new antibacterial and antitumor agents, we have prepared new analogues pteroic acid(13a, 13b), which means C-9 position of pteroic acid has been replaced by norfloxacin(8) or ciprofloxacin(9) and amino group of C-2 position by $CH_3$. These derivatives were synthesized coupling at N-4 piperazine of norfloxacin and ciprofloxacin with 2-amino-3-cyano-5-chloromethylpyrazine(20) provided 1-alkyl(ethyl, cyclopropyl)-6-fluoro-1,4-dihydro-4-oxo-7-[[4-N-(2-amino-3-cyanopyrazin-5-yl)methyl]piperazin-1-yl]-3-quinoline-carboxylic acid(12a, 12b). It was then cyclized with acetamidine. HCI to obtain new analogues of C-2 desaminomethylpteroic acid(13a, 13b) in yield of 76.2% and 82.8 % respectively. These compounds were tested in vitro on antibacterial activity against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa ATCC9027. In general, these synthesized compounds(13a, 13b) showed less potent activities than those of norfloxacin.

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The Components of the Fermented Soy Sauce from Gorosoe and Bamboos SaP (고로쇠 및 대나무 수액간장의 성분조성)

  • 정미자;조종수;김행자;성낙주
    • The Korean Journal of Food And Nutrition
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    • v.14 no.2
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    • pp.167-174
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    • 2001
  • Soy sauce was prepared with the addition of Gorosoe and bamboos sap instead of tap water to make ordinary soy sauce, respectively. The changes of such compounds during fermentation as minerals, free sugars, organic acids and free amino acids were analyzed. Total mineral contents in the 90 days fermented soy sauce from Gorosoe and bamboos sap were increased by 2.0 and 4.4 times as compared with those of control samples, respectively. Especially the increase of calcium, potassium and magnesium in soy sauce of sapes were derived from those of saps. The sugars were found to be only glucose and galactose in control samples, but they were detected not only above sugar but also fructose and sucrose in soy sauce of saps. Butyric acid in detected organic acid were dominant in all stray sauce samples. In the free amino acid composition of control samples, leucine, phenylalanine, isoleucine, lysine and glutamic acid were abundant amino acids. Amino acid such as isoleucine, leucine and phenylalanine were decreased, the rest 11 kinds of amino acids containing phosphoserine were increased during the fermentation of control samples. Increasing and decreasing patterns of free amino acids during fermentation of sap soy sauce were similar to control samples. Total nitrogen, amino acid nitrogen and ammonia nitrogen were increased during their fermentation.

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Novel Two-dimensional Network Based on Amino-acid-octamolybdate Bridged by Second Metals: {M(H2O)3(pro)Mo4O13}2·2H2O (pro = proline, M = Co, Ni, Cu, Zn)

  • Wu, Xiao-Yuan;Lu, Can-Zhong;Xia, Chang-Kun;Chen, Shu-Mei;Liu, Jiu-Hui;Chen, Li-Juan;Yang, Wen-Bin
    • Bulletin of the Korean Chemical Society
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    • v.27 no.8
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    • pp.1206-1210
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    • 2006
  • Four isostructural amino-acid-based polyoxomolybdates, {$M(H_2O)_3(pro)Mo_4O_{13}$}$_2{\cdot}2H_2O$ (pro = proline, M = Co (1), Ni (2), Cu (3), Zn (4)), have been synthesized and structurally characterized by single crystal X-ray diffraction, elemental analysis, IR spectrum, TG analysis. The structures of 1-4 are layered networks built up from {$Mo_8O_{26}(pro)_2$}$^{4-}$ units and {$M(H_2O)_3O_3$} octahedra, the uncoordinated water molecules occupying the interlayer regions.

The Stability of TPN Admixture of Amino acids Solution and Dextrose Solution (고영양수액요법에 빈용되는 아미노산수액제와 포도당액의 혼합시 안정성에 관한 연구)

  • Song, Mi Kyeong;Suh, Ok kyung;Lee, Suk Hyang;Lee, Sung Woo;Shin, Hyun Taek
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.147-158
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    • 1998
  • The purpose of this study was to test the stability of TPN basic solutions containing amino acids and dextrose. Test solutions containing $4.25\%$ amino acids in $25\%$ dextrose (central TPN basic solution) or $4.25\%$ amino acids in $10\%$ dextrose (peripheral TPN basic solution) were prepared. Two different amino acids solutions $(Fravasol^{(R)}\;vs\;Freamine^{(R)})$ were tested. The samples were taken from each admixture and stored in the evacuated, sterile containers at $2{\sim}8^{\circ}C$ and ambient room temperature. Each sample was analyzed at 0, 3, 7, 14 and 30 days of storage. Each amino acid was analyzed by amino acid analyzer. Dextrose content was measured by polarimeter. The pH and chromagen formation were also monitored. The decomposition was measured by the changes in concentration of amino acids and dextroser TPN basic $solution-Freamine^{(R)}$ admixture stored at $2\sim8^{\circ}C$ were stable for 30 days. Central and peripheral TPN basic solutions stored at room temperature were stable for 7 days and 14 days, respectively. There were no changes in color for 30 days by naked eye. Amino acid concentrations in TPN basic $solution-Fravasol^{(R)}$ admixture stored at $2\sim8^{\circ}C$ or room temperature were stable for 30 days. But, significant color change was detected according to passing time. In conclusion, Peripheral TPN basic $solution-Fravasol^{(R)}$ admixture stored at room temperature and in refrigerator were stable for 3 days and 7 days, respectively. However, central TPN basic solution-Fravasol admixtures were unstable. Therefore, it is recommended that it should be admixed right before use.

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Facile Synthesis of (2S,3R)-3-Amino-2-hydroxy-4-(4'-hydroxyphenyl)butanoic Acid. Application to the Synthesis of Inhibitors of Aminopeptidases

  • Moon, Byung-Jo;Huh, Kyung-Lan
    • Bulletin of the Korean Chemical Society
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    • v.12 no.1
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    • pp.71-74
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    • 1991
  • Facile methods are reported for the synthesis of optically pure derivatives of (2S,3R)-3-amino-2-hydroxy-4-(4'-hydroxyphenyl)b utanoic acid. To avoid troublesome synthesis of O-benzyl-N-Boc-D-tyrosine, without the protection of phenolic OH group of tyrosine N-Boc-D-tyrosine methyl ester was reduced with DiBAL to the aldehyde. The aldehyde was converted via the cyanohydrin to (2S,3R)-3-amino-2-hydroxy-4-(4'-hydroxyphenyl)butanoic acid (AHpHBA). The mixture of diastereomers was converted to the corresponding Boc-AHpHBA methyl ester derivatives and separated by chromatography over silica gel. Optically active (2S,3R)-AHpHBA was used to synthesize aminopeptidase inhibitors.

The Variation of the Contents of Free Amino Acids and the Carbohydrates in the Whole Plant of Fagopyrum escullentum Moench during the Stages of Growing (모밀(Fagopyrum esculentum Moench)생장과정중의 유리 Amino 산과 당질의 성장에 관하여)

  • 황희자
    • YAKHAK HOEJI
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    • v.8 no.2
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    • pp.48-53
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    • 1964
  • At the different growing stages of Fagopyrum esculentum Moench planted at the green house and out doors, the contents of free amino acids in the whole plants,were determined quantitatively by spot-extract colorimetric method (J. Awapara method) using the chromatograms obtained by the ion-exchange resin and paper chromatographic method. And the contents of carbohydrate in the whole plant were determined by Bertrand method. The results were summarized as follows. 1. Almost same kinds of free amino acids were detected in the both plants. 2. Concentrations of most amino acids was increased progressively during growth; further growth was accompanied by decreased concentrations. 3. Rate of growth and increasing of total amino acid content of green house plant is greater than that of out dorrs plant. 4. At the same stages of gwoth, total free amino acid content of green house plant is higher than that of out doors plant but sugar content is lower. 5. There was rapidly increasing of sugar content and decreasing of total free amino acid content except asparagine during mature of seeds.

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Delayed Deproteinization Causes Methodological Errors in Amino Acid Levels in Plasma Stored at Room Temperature or -20℃

  • Li, Junyou;Piao, Chunxiang;Jin, Huazi;Wongpanit, Kannika;Manabe, Noboru
    • Asian-Australasian Journal of Animal Sciences
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    • v.22 no.12
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    • pp.1703-1708
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    • 2009
  • Deproteinization has been recognized as a prerequisite for amino acid analysis of plasma samples. For plasma stored at room temperature, delaying deproteinization for 30, 60 or 120 minutes did not result in significant changes in the mean CV (coefficient of variation), which ranged from 4.4 to 5.6%. However the mean CV of aspartic acid, ${\alpha}$-aminoadipic acid, alanine and lysine was about 10%. When the plasma was stored frozen at -20${^{\circ}C}$, the CV was increased at 0 and 120 minutes after thawing, to 12.4% (range, 4.1 to 35.3%) and 8.0% (2.5 to 30.7%), respectively. The concentrations in plasma during storage at room temperature of all the amino acids analyzed showed significant changes. In plasma stored for 30 minutes at room temperature, 17 amino acids increased in concentrations and two decreased. Extending this period to 60 or 120 minutes increased the instability as compare to the reference group. Storing plasma at -20${^{\circ}C}$ for 2 weeks resulted in significantly greater changes in the amino acid concentrations than at room temperature. On extending the storage time at room temperature, after thawing, to 30, 60, and 120 minutes, 21, 20, and all 22 amino acids respectively changed significantly (p<0.01). The present study indicates that methodological errors occur in the concentrations determined for all amino acids when plasma is left at room temperature. The storage of frozen non-deproteinized plasma accompanied more significant changes in most amino acid concentrations and thus should be avoided. Deproteinization should be performed as soon as possible after plasma collection.

Crystal structure of 1-tert-butoxycarbonyl-4-[N-(tert-butoxycarbonyl)-N-(ethoxycarbonylmethyl)amino]-3-phenylsulfonylpyrrolidind (1-tert-butoxycarbonyl-4-[N-(tert-butoxycarbonyl)-N-(ethoxycarbonylmethyl)amino]-3-phenylsulfonylpyrrolidind의 결정구조해석)

  • 조소라;김문집
    • Korean Journal of Crystallography
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    • v.6 no.1
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    • pp.27-35
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    • 1995
  • The crystal structure of 1-tert-butoxycarbonyl-4-[N-(tert-butoxycarbonyl)-N-(ethoxycarbonylmethyl)amino]-3-phenylsulfonylpyrrolidind [C24H36O8N2S] has been from single crystal x-ray diffraction study ; C24H36O8N2S triclinic, p1, a=11.363(8)Å, b=11.589(6)Å, c=11.013(10)Å,α=95.32(6)°,β=98.64(7)°,γ=79.57(5)°,V=1406.8(18)Å3, t=293K, Z=2, CuKα(λ=1.5418Å). The molecular structure was solved by diredt method and refined by full-matrix least squares to a final R=9.78% for 3621 unique observed [F≥4σ(F)] reflections and 703 paramenters.

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