• Title/Summary/Keyword: 4-Amino-2

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Synthesis of Some Biologically Active Halogenopurines (생물 활성이 있는 Halogenopurines의 합성)

  • Hu, Yu Lin;Liu, Xiang;Lu, Ming;Ge, Qiang;Liu, Xiao Bin
    • Journal of the Korean Chemical Society
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    • v.54 no.4
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    • pp.429-436
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    • 2010
  • A series of some biologically active halogenopurines were synthesized from commercially available guanine (1). The reaction of guanine with acetic anhydride yielded 2,9-diacetylguanine (2-1) by acetylation reaction. Further treatment of 2-1 with $POCl_3$ by PEG-2000 phase transfer catalysis furnished the important compound 3a, then 2-amino-6-halogenopurines (3b-d) were obtained through chlorine-exchange halogenations between KX and 3a by TPPB phase transfer catalyst. Further, 2-halogenopurines (2-2a-d, 4-2a-d, 5a-d) were efficiently prepared from 2-amino-6-substituted purines (1, 3a, 4-1) via a diazotization catalyzed by their corresponding CuX, and some new compounds 2-2a, 2-2c, 2-2d, 4-2c, 4-2d, 5b, 5c and 5d have been discovered. The structures of synthesized compounds were mainly established on the basis of their elemental analysis, $^1H$ NMR, as well as their mass spectral data. All the title compounds were screened for their antifungal activities, and some of the compounds showed promising activity.

Chemical composition and Stabilities of Invertase from Korean Ginseng, Panax ginseng (고려인삼(Panax RiwenR) Invertase의 화학조성과 안정성)

  • 김용환;김병묵
    • Journal of Ginseng Research
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    • v.14 no.1
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    • pp.21-26
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    • 1990
  • The chemical composition and stabilities of the purified ginseng invertase were investigated. The purified enzyme was found to be a glycoprotein composed of 80.2% protein and 19.7% total sugar. The protein component of the enzyme was composed of acidic amino acid (9.3%), basic amino acid (48.9%), nonpolar amino acid (21.4%), polar amino acid (20.4%) and 6.1% S-containing amino acid. It showed especially high contents of histidine and serine. The enzyme was inactivated almost completely by the treatment with some proteases (papain, pepsin. trypsin, pancreatin and microbial alkaline pretense) and protein denatllrants (8M urea and 6M guanidine-HC1), bolt not with glyrosidase (${\alpha}$-amylase, ${\beta}$-amylase. glcoamylese and cellullase). btonosaccharides sllch as glilrose, fructose, galactose and mannose did not exert any influence on the enzyme activity. The activity of the enzyme was inhibited by Ag+, Mn2+, Hg2+, Zn2+ and Al3+, whereas Ca2+, Mg2+, Ba2+ and Fe3+ gave rather activating effects on the enzyme activity. The enzyme was relatively stable in the VH range of VH 6 and 8, and at the temperatures below 35$^{\circ}C$.

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Sulphur Supply Level Effects on the Assimilation of Nitrate and Sulphate into Amino Acids and Protein in Forage Rape (Brassica napus L.)

  • Lee, Bok-Rye;Kim, Tae-Hwan
    • Journal of The Korean Society of Grassland and Forage Science
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    • v.32 no.4
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    • pp.343-352
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    • 2012
  • Sulphur deficiency has become widespread over the past several decades in most of the agricultural area. Oilseed rape (Brassica napus L.) is a very sensitive to S limitation which is becoming reduction of quality and productivity of forage. Few studies have assessed the sulphur mobilization in the source-sink relationship, very little is known about the regulatory mechanism in interaction between sulphur and nitrogen during the short-term sulphur deficiency. In this study, therefore, amount of sulphur and nitrogen incorporated into amino acids and proteins as affected by different S-supplied level (Control: 1 mM ${SO_4}^{2-}$, S-deficiency: 0.1 mM ${SO_4}^{2-}$, and S-deprivation: 0 mM ${SO_4}^{2-}$) were examined. The amount of sulphur in sulphate (S-sulphate) was significantly decreased by 25.8% in S-deprivation condition, compare to control, but not nitrogen in nitrate (N-nitrate). The markedly increase of sulphur and nitrogen incorporated amino acids (S-amino acids and N-amino acids) was observed in both S-deficiency and S-deprivation treatments. The amount of nitrogen incorporated proteins (N-protein) was strongly decreased as sulphur availability while the amount of sulphur incorporated into proteins (S-protein) was not affected. A highly significant ($p{\leq}0.001$) relationship between S-sulphate and S-amino acid was observed whereas the increase of N-amino acids is closely associated with decrease of N-proteins. These data indicate that increase of sulphur and nitrogen incorporated into amino acids was from different nitrogen and sulphur metabolites, respectively

Plasma Amino Acid Status of Crossbred Heifers Fed Two Levels of Dietary Protein and its Relationship to Puberty Onset

  • Swain, R.K.;Kaur, Harjit
    • Asian-Australasian Journal of Animal Sciences
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    • v.15 no.12
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    • pp.1714-1718
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    • 2002
  • Twelve prepubertal Karan Fries heifers (15 months, $167.7{\pm}13.5kg$) were divided into two equal groups. Group 1 was fed as per NRC requirements and group 2 was fed 20% more protein than group 1 heifers. The experimental feeding was continued until the onset of puberty in both the groups. Blood samples were collected at fortnightly intervals and analyzed for amino acids using HPLC. Group 1 and 2 heifers required $178.6{\pm}33.8$ and $152.8{\pm}33.2$ days of experimental feeding to exhibit first estrus resulting in total age at puberty as $639.4{\pm}27.3$ and $618.6{\pm}24.6$ days in the two groups respectively. The concentration of total amino acids averaged 4.40 and 4.89 mmol/l and those of non-essential amino acids (NEAA) was 2.32 and 2.49 mmol/l in groups 1 and 2, respectively. The concentration of plasma essential amino acids i.e. histidine, threonine, valine, methionine, isoleucine, leucine and phenylalanine were higher (p<0.01) in group 2 than group 1. Plasma concentration of large neutral amino acids (LNAA) was significantly higher in group 2 (1.28 mmol/l) than in group 1 (1.12 mmol/l). Increased levels of leucine, isoleucine and valine are implicated in increased follicular growth and development in prepubertal heifers and resulted in a 26 day earlier attainment of puberty by 26 days in an experimental period of six months in group 2 heifers. Increased concentrations of aspartate and tyrosine in group 2 heifers might be associated with the release of GnRH from the hypothalamus influencing LH release from anterior pituitary in such animals. It is therefore evident that increased availability of certain amino acids in heifers fed high protein diet might have led to early onset of puberty.

Synthetic Studies on Fused Nitrogen-heterocycles from N-Amino-N,N '-dihydrodiazinediones (II). Condensation of N-Amino-N,N '-dihydrodiazinediones with ${\alpha},{\beta}$-Unsaturated Carbonyl Compounds

  • Sung Chul Shin;Kyung Ho Kang;Youn Young Lee;Yang Mo Goo
    • Bulletin of the Korean Chemical Society
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    • v.11 no.1
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    • pp.22-25
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    • 1990
  • The condensation of 1-amino-1,2-dihydro-3,6-pyridazinedione (1) and 2-amino-2,3-dihydro-1,4-phthalazinedione (2) with mesityl oxide or 3-penten-2-one in acetic acid-ethanol (1:1) gave 3,4,6,9-tetrahydro-6,9-dioxopyridazino[1,2-a][1,2, 3]triazines (9,11) and 3,4,6,11-tetrahydro-6,11-dioxo[1,2,3]triazino[1,2- b]phthalazines (10,12), respectively. The condensation of 1 and 2 with crotonaldehyde, cinnamaldehyde or acrylaldehyde under the same reaction condition gave only N-alkylidene derivatlives (3-8). When the N-alkylidene derivatives isolated from the reaction of 1 and 2 with crotonaldehyde and cinnamaldehyde (3-6) were refluxed in acetic acid, the corresponding heterocyclic compounds (13-16) were obtained.

Synthesis and Biological Evaluation of Novel 2-[Substituted acetly]-amino-5-alkyl]-amino-5-alkyl-1,3,4-thiadiazoles

  • Shakya, Ashok K.;Mishra, Pradeep;Patnaik, G.K.;Shukla, Rakesh;Srimal, R.C.
    • Archives of Pharmacal Research
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    • v.21 no.6
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    • pp.753-758
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    • 1998
  • Sixteen novel 2-substituted acetyl amino-5-alkyl-1,3,4-thiadiazol were synthesized and screened for their pharmacological activities. A few of the compounds namely 11, 12 and 16 showed anti-inflammatory activities comparable to phenylbutazone. Compound 12 also showed significan non-specific spasmolytic activity. Diuretic activity of compound 15 at a dose level of 90mg/kg p.o. was two fold higher compared to 50mg/kg p.o. of furosemide. Comparable diuresis was aso produced by compounds 9, 10, and 16.

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Extractive Nitrogenous Constituents and Their Monthly Variation of Fresh Laver Porphyra dentata (잇바디돌김의 함질소 엑스성분조성 및 월별변동)

  • 박춘규;박철훈;박정임
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.30 no.4
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    • pp.579-588
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    • 2001
  • In order to investigate the composition and monthly variation of extractive nitrogenous components in the laver Porphyra dentata cultured at the south coast of Korea, the fresh laver was analyzed separately for the amounts of free amino acids, combined amino acids, ATP and its related compounds, and quaternary ammonium basis in fresh laver were measured. The extractive nitrogen contents of fresh laver extracts were 760~870 mg/100g (dry basis). Twenty-seven to thirty-one kinds of free amino acids were detected in the laver extracts and their total amounts were 2,404~3,966 mg/100g (on dry basis). The laver extracts showed rich in free amino acids such as alanine, taurine, glutamic acid, glutamine and aspartic acid. Sixteen to twenty-three kinds of combined amino acids were detected in the extracts and their total amounts were 1,429~2,692 mg/100g (on dry basis). Proline, glutamic acid, glycine, phosphoserine, serine were the amin combined amino acids in the extracts. The amounts of ATP and related compounds were 73.3~94.4 mg/100 g (2.04~4.43 $\mu$mol/g, on dry basis). Homarine and trigonelline were detected in all specimens but $\beta$-alaninebetaine, ${\gamma}$-butyrobetaine were found in some. Small amounts of trimethylamine were detected in all samples. Free and combined amino acids were occupying almost 90% of extractive nitrogen. Most of free and combined amino acids showed a marked monthly variation with a maximum in January and March, and a minimum in February and April. The fresh laver P. dentata did not differ much from the fresh laver P. yezoensis in qualitative com-position of extractive components, but their contents were generally low level.

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Synthesis, Fastness and Spectral Properties of Some New Azo Pyrazole and Pyrazolotriazole Derivatives (Pyrazole과 Pyrazolotriazole 유도체의 합성 및 특성 연구)

  • Rizk, Hala F.;El-Badawi, Mahmoud A.;Ibrahim, Seham A.;El-Borai, Mohamed A.
    • Journal of the Korean Chemical Society
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    • v.54 no.6
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    • pp.737-743
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    • 2010
  • Coupling of 5-amino-1,3-diaryl-pyrazoles 1a-c with diazonium salts of different aryl amines gave a series of novel 1,3-diaryl-5-amino-4-arylazopyrazoles 3a-l. Such compounds could be also obtained by reaction of 5-amino-1,3-diaryl-4-nitroso- 1H-pyrazoles 2a-c with different aryl amines in alkaline medium. Oxidation of azo derivatives 3a-l with cupric acetate, in dimethyl formamide and stream of air, gave 2,4,6-triaryl-2,4-dihydropyrazolo [4,3-d]-1,2,3-triazoles 4a-l. and the fluorescence properties of the cyclic triazoles were studied. Diazotization of 5-amino-1,3-diaryl-1H-pyrazoles 1a-c by sodium nitrite in ortho-phosphoric acid followed by coupling with some aryl amines gave o-aminoazo compounds 5a-f. Cyclisation of compounds 5a-f in pyridine and cupric acetate gave the corresponding triazoles 6a-f. The coupling of compounds 6a-f with different aryl diazonium salts gave compounds 7a-j. The synthesized dyes were applied to polyesters as disperse dyes and the fastness properties were evaluated.

Performance of Broiler Chickens Fed Low Protein, Limiting Amino Acid Supplemented Diets Formulated Either on Total or Standardized Ileal Digestible Amino Acid Basis

  • Kumar, C. Basavanta;Gloridoss, R.G.;Singh, K.C.;Prabhu, T.M.;Suresh, B.N.
    • Asian-Australasian Journal of Animal Sciences
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    • v.29 no.11
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    • pp.1616-1624
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    • 2016
  • The aim of present experiment was to investigate the effect of protein reduction in commercial broiler chicken rations with incorporation of de-oiled rice bran (DORB) and supplementation of limiting amino acids (valine, isoleucine, and/or tryptophan) with ration formulation either on total amino acid (TAA) or standardized ileal digestible amino acids (SIDAA). The experimental design consisted of $T_1$, TAA control; $T_2$ and $T_3$, 0.75% and 1.5% protein reduction by 3% and 6% DORB incorporation, respectively by replacing soybean meal with supplemental limiting amino acids to meet TAA requirement; $T_4$, SIDAA control, $T_5$ and $T_6$, 0.75% and 1.5% protein reduction by DORB incorporation (3% and 6%) with supplemental limiting amino acids on SIDAA basis. A total of 360 dold fast growing broiler chicks (Vencobb-400) were divided into 36 homogenous groups of ten chicks each, and six dietary treatments described were allocated randomly with six replications. During 42 days trial, the feed intake was significantly (p<0.05) reduced by TAA factor compared to SIDAA factor and protein factor significantly (p<0.05) reduced the feed intake at 1.5% reduction compared to normal protein group. This was observed only during pre-starter phase but not thereafter. The cumulative body weight gain (BWG) was significantly (p<0.05) reduced in TAA formulations with protein step-down of 1.5% ($T_3$, 1,993 g) compared to control ($T_1$, 2,067 g), while under SIDAA formulations, BWG was not affected with protein reduction of 1.5% ($T_6$, 2,076 g) compared to $T_4$ (2,129 g). The feed conversion ratio (FCR) was significantly (p<0.05) reduced in both TAA and SIDAA formulations with 1.5% protein step-down ($T_3$, 1.741; $T_6$, 1.704) compared to respective controls ($T_1$, 1.696; $T_4$, 1.663). The SIDAA formulation revealed significantly (p<0.05) higher BWG (2,095 g) and better FCR (1.684) compared to TAA formulation (2,028 g; 1.721). Intake of crude protein and all limiting amino acids (SID basis) was higher in SIDAA group than TAA group with resultant higher nitrogen retention (4.438 vs 4.027 g/bird/d). The nitrogen excretion was minimized with 1.5% protein reduction (1.608 g/bird) compared to normal protein group (1.794 g/bird). The serum uric acid concentration was significantly reduced in $T_3$ (9.45 mg/dL) as compared to $T_4$ (10.75 mg/dL). All carcass parameters were significantly (p<0.05) higher in SIDAA formulation over TAA formulation and 1.5% protein reduction significantly reduced carcass, breast and thigh yields. In conclusion, the dietary protein can be reduced by 0.75% with TAA formulation and 1.5% with SIDAA formulation through DORB incorporation and supplementation of limiting amino acids and among formulations, SIDAA formulation was better than TAA formulation.

Comparative Studies on the Composition of Korean Human and Cow's Milk (I) -Amino Acid Composition of Human and Cow's Milk of Korea- (한국인(韓國人) 모유(母乳)와 우유(牛乳)의 성분(成分) 조성(組成)에 관(關)한 비교(比較) 연구(硏究) (I) -한국인(韓國人) 모유(母乳)와 우유중(牛乳中)의 Amino산(酸) 조성(組成)에 관(關)한 연구(硏究)-)

  • Ko, Young-Su;Kim, Jung-Ja;Han, In-Ja
    • Journal of Nutrition and Health
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    • v.3 no.2
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    • pp.87-94
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    • 1970
  • The amino acid composition of human and cow's milk represents a standard of reference in infantnutrition. The amino acid compositions determined by automatic amino acid analyzer, Yanagimote Model LC-5. Protein in the human and cow's milk were found to be hydrolyzed to yield free amino acids. Qualitative data for free amino acids in the milk are as follows: 1) Amounts of acidic amino acids such as glutamic and aspartic acid in cow's milk were obserbed to be about 2 times compared with human milk and it is considered that the abundance in these amino acids may contribute significantly to the specific flavor of cow's milk. 2) It is much interesting that in the human milk the contents of sulfur-containing amino acids were high comparatively better than cow's milk; cystine was found to be 3 times ana methionine, 2 times. 3) In the human milk a high content of some essential amino acids such as threonine, isoleucine and leucine was demonstrated and a specific flavor sweet amino acids. 4) Large amounts of basic amino acid such as histidine was found to occur in human milk and arginine in cow's milk.

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