• Title/Summary/Keyword: 5-Amino-3H-1

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Heterocyclic Systems Containing Bridgehead Nitrogen Atom:Synthesis and Evaluation of Biological Activity of Imidazo[2,1-b]-1,3,4-thiadiazolo [2,3-c]-s-triazoles, s-Triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]quinoxaline and bis-(s-Triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b][imidazo[4,5-b]-cyclohexane]-5a,6a-diene)

  • Kumar, Parvin;Kuamr, Ashwani;Mohan, Late Jag;Makrandi, J.K.
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3304-3308
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    • 2010
  • Condensation of 4-amino-5-mercapto-3-($\alpha$-naphthyl)-s-triazole (1) with cyanogen bromide gives 6-amino-3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazole (2) which on condensation with chloranil yields 3,9-di-($\alpha$-naphthyl)-6,14-dioxo-bis-(s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]cyclohexane]-5a,6a-diene) (3). 3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]quinoxaline (4) is obtained by a similar condensation of (2) with 2,3-dichloroquinoxaline. The reaction of (2) with $\alpha$-haloketones followed by bromination affords 7-aryl-3-($\alpha$-naphthyl)-imidazo[2,1-b]-1,3,4-thiadiazolo[2,3-c]-s-triazoles (5) and their 6-bromo analogues 6 respectively. The structures of all newly synthesized compounds were established on the basis of elemental analyses, IR, $^1H$-NMR. The antibacterial and antifungal activities of all newly synthesized compounds have also been evaluated.

Synthesis and Pharmacological Studies of Some Pyrone and Benzodifuran Derivatives

  • Hishmat, Orchidee H.;El-Diwani, Hoda I.;Bakr, Sherifa M.A.;Mahmoud, Sawsan S.;Nada, Somaya A.
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.168-174
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    • 1993
  • The michael adducts 2a, b were obtained from the reaction of the phenylacelyl derivative 1 with benzadehyde and p-anisaldehyde and p-anisaldehyde respectively. 2a and 2b were subjected to react with cyanoethanoic acid hydrazide, malononitrile, cyanothioacetamide, cyanoacetamide and 1, 1, 3-tricyano-2-amino propene to yield 4a-h and 5a, b respecitively. Hydrogen peroxide oxidation of 2a, b gave the aurone derivative 6a, b. The pyone derivatives 8a, b were obtained from 2a, b by addition of chioroacetyl chioride followed by dehydrochlorination.

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Effect of Essential and Nonessential Amino Acids in North Carolina State University (NCSU)-23 Medium on Development of Porcine In vitro Fertilized Embryos

  • Hashem, Md. Abul;Bhandari, Dilip P.;Hossein, Mohammad Shamim;Jeong, Yeon Woo;Kim, Sue;Kim, Ji-Hye;Koo, Ok-Jae;Park, Seon Mi;Lee, Eu Gine;Park, Sun Woo;Kang, Sung Keun;Lee, Byeong Chun
    • Asian-Australasian Journal of Animal Sciences
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    • v.20 no.5
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    • pp.693-700
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    • 2007
  • The present study was conducted to examine the effect of different levels of essential and nonessential amino acid in NCSU-23 medium on the in vitro-produced porcine embryo as it develops from the zygote to the blastocyst stage. Four experiments were performed, each with a completely randomized design involving 5 to 8 replications of treatments. In order to know the effect of nonessential amino acids in NCSU-23 medium, 0, 5, 10 and $20{\mu}/ml$ MEM were supplemented there to, (Exp. 1) and the medium was supplemented with same level of essential amino acids (Exp. 2). The combined effect of nonessential (0, 5, 10 and $20{\mu}/ml$ MEM) and essential amino acids (0, 5, 10 and $10{\mu}/ml$ MEM) in NCSU-23 medium (Exp. 3), first 72 h with non-essential amino acids (at 0, 5, 10 and $20{\mu}/ml$ MEM), and last 4 d with essential amino acids with the same level as NEAA (Exp. 4) were examined. The embryo development was monitored and the quality of blastocysts was evaluated by counting the number of total cells and determining the ratio of inner cell mass (ICM) to trophoectoderm (TE) cells. When Eagle's nonessential amino acids (MEM) added to NCSU-23 medium, it significantly increased the likelihood of development to the 2- to 4-cell stage and subsequent blastocyst development. Supplementation of different levels of essential amino acids in the NCSU-23 medium decreased cleavage rate, rate of morula and blastocyst development and the number of ICMs. In the case of the combined effect of essential and nonessential amino acids, better and significant results were found for blastocysts, hatching blastocysts and for ICM numbers which were also dose dependent. With respect to the biphasic effect of nonessential and essential amino acids, nonessential amino acids increased cleavage whereas essential amino acids increased the total cell number. Neither the nonessential nor the essential group of amino acids, on their own, affected blastocyst cell number or the differentiation of cells in the blastocyst. In conclusion, this study determined the role of nonessential and essential amino acids in the culture of the porcine embryo and showed that the embryo requires different levels of amino acids as it develops from the zygote to the blastocyst stage.

Dyeing of Nylon/Cotton Blend with Acid Dyes Using Sodium 2-(2,3- dibromopropionylamino)-5-(4,6-dichloro-1,3,5-triazinylamino)-benzenesulfonate (Sodium 2-(2,3-dibromopropionylamino)-5-(4,6-dichloro-1,3,5-triazinylamino)-benzenesulfonate를 이용한 나일론/면 복합소재의 단일 산성염료 일욕염색)

  • Kim, Mi-Kyung;Yoon, Nam-Sik;Kim, Tae-Kyeong
    • Textile Coloration and Finishing
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    • v.24 no.1
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    • pp.8-17
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    • 2012
  • In order to dye nylon/cotton blended fabrics in solid colors with only acid dyes, a hetero-bifunctional bridge compound (DBDCBS) was examined. The bridge compound was designed to react only onto cotton fabrics first, on which amino-containing acid dyes react later by covalent bonding. By the effect of DBDCBS, amino-containing acid dyes exhibited high affinity toward the cotton fabrics. From the dyeing properties examined at various conditions, the optimum dyeing was decided at pH 4 and $100^{\circ}C$. Consequently, the solid color was obtained on nylon/cotton blended fabrics in one bath dyeing process using only acid dyes. The DBDCBS did not show any negative effect on nylon side in terms of dyeing and physical properties.

Effect of Amino Acids Supplemented to Culture Medium on Development of Porcine Embryos Culturde in Vitro (아미노산의 첨가가 돼지 체외수정란의 후기배의 발달에 미치는 영향)

  • Kim Y. S.;Song S. H.;Cho S. K.;Kwack D. O.;Kim C. W.;Park C. S.;Chung K. H.
    • Reproductive and Developmental Biology
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    • v.29 no.3
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    • pp.201-205
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    • 2005
  • The objective of this study was to investigative the effects of amino acids supplementation on maturation, fertilization and embryo development of pig oocytes. Essential amino acids (EA), non-essential amino acids (NA) or both amino acids (EA + NA) were supple-mented to North Carolina State University (NCSU) 23 medium containing porcine follicular fluid (pFF). When the amino acids were supplemented to the maturation medium, the maturation rates were higher (p<0.05) in the NA group than control ($83.3{\pm}0.04\%\;versus\;70.0{\pm}0.05\%$, but the subsequent cleavage rates and development to morula and blstocyst stage between aminoacid supplement groups and control were not different. The developmental rates to morula and blastocysts stage were not significantly different regardless of amino acid supplementation to culture medium. In addition, supplementation of amino acids did not significantly affect the rate of fertilization and polyspermy. When the amino acids were supplement to culture medium, the number of trophectodermal (TE) cells was significantly (p<0.05) higher in amino acid supplement group than that of control ($18.6{\pm}0.5\;versus\;16.1{\pm}0.6$), whereas the numbers of inner cell mass (ICM) cells were not different among the treaonent groups and control ($29.0{\pm}0.9\~31.5{\pm}1.2$). Total cell number was also significantly (p<0.05) higher in EANA group ($50.0{\pm}1.0$) than that of control group ($44.2{\pm}1.1$). These results indicate that the amino acid supplementation to maturation and culture medium may not significantly stimulate early embryo development, but may improve the TE cell number of blastocyst stage in the pig.

In Vitro Metabolism of a New Neuroprotective Agent, KR-31543 in the Human Liver Microsomes : Identification of Human Cytochrome P450

  • Ji, Hye-Young;Lee, Seung-Seok;Yoo, Sung-Eun;Kim, Hosoon;Lee, Dong-Ha;Lim, Hong;Lee, Hye-Suk
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.239-245
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    • 2004
  • KR-31543, (2S,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(2 -methyl-2H-tetrazol-5-ylmethyl) amino]-3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-1-benzopyran, is a new neuroprotective agent for preventing ischemia-reperfusion damage. This study was performed to identify the metabolic pathway of KR-31543 in human liver microsomes and to characterize cytochrome P450 (CYP) enzymes that are involved in the metabolism of KR-31543. Human liver microsomal incubation of KR-31543 in the presence of NADPH resulted in the formation of two metabolites, M1 and M2. M1 was identified as N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine on the basis of LC/MS/MS analysis with a synthesized authentic standard, and M2 was suggested to be hydroxy-KR-31543. Correlation analysis between the known CYP enzyme activities and the rates of the formation of M 1 and M2 in the 12 human liver microsomes have showed significant correlations with testosterone 6$\beta$-hydroxylase activity (a marker of CYP3A4). Ketoconazole, a selective inhibitor of CYP3A4, and anti-CYP3A4 monoclonal antibodies potently inhibited both N-hydrolysis and hydroxylation of KR-31543 in human liver microsomes. These results provide evidence that CYP3A4 is the major isozyme responsible for the metabolism of KR-31543 to M1 and M2.

Changes in the Contents of Sugar, Organic Acid, Free Amino Acid and Nucleic Acid-Related Compounds during Fermentation of Leaf Mustard-Kimchi (갓김치 숙성중 당, 유기산, 유리아미노산 및 핵산관련 물질 함량의 변화)

  • 박석규;조영숙;박정로;문주석;이용수
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.24 no.1
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    • pp.48-53
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    • 1995
  • Changes in the contents of sugar, organic acid, free amino acid and uncleic acid-related compounds of leaf mustard-Kimchi during fermentation at 5~7$^{\circ}C$ were investigated. The leaf mustard-Kimchi was formulated with 4kg leaf mustard, 120g garlic, 80g ginger, 540ml salted anchovies, 1kg green onion, 200g red pepper powder, 200g ground red pepper, 60g whole sesame and 600ml glutinous rice paste. Changes in pH and acidity were relatively slow. Major free sugars were glucose(0.13%) and maltose(0.42%), and residual sugars(0.03-0.04%) were also detected after 32 days of fermentation. Major free amino acids containing more than 26.5mg% were proline, glutamic acid, alanine and histidine. Contents of total free amino acids increased from 244.8 to 397.2mg% by 24 days of fermentation. Of non-volatile organic acid, lactic acid was the most abundant(119.3mg%), and its content increased markedly after 10 days of fermentation. Other organic acids(below 53.1mg%) observed were malic, oxalic and citric acid. Contents of nucleic acid-related compounds were high in the order of hypoxanthine(22.8mg%), IMP(8.3mg%) and GMP(6.9mg%). Hypoxanthine content increased by 10 days(27.3mg%) and decreased thereafter, while the others decreased gradually during the overall period of fermentation.

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Synthesis of Some Imidazopyrazolopyrimidines, Pyrazolopyrimidopyrimidines and Pyrazolopyrimidothiazines

  • Elkhawaga, A.M.;Kamal El-Dean, A.M.;Radwan, M.;Ahmed, M.M.
    • Bulletin of the Korean Chemical Society
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    • v.30 no.3
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    • pp.561-566
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    • 2009
  • Chloroacylation of 3-amino-2-phenylpyrazole-4-carboxamide (2) using chloroacetyl-(propionyl) chloride affording 6-chloromethyl(ethyl)-1-phenylpyrazolo[3,4-d]pyrimidin-4[5H]-one (3) or (6). Chlorine atom in compound (3) or (6) underwent nucleophilic substitution reaction with primary or secondary amines to give 6-alkyl(aryl)aminomethyl(ethyl)-1-phenylpyrazolo[3,4-d]pyrimidin-4[5H]-one (4a-g,7a-f). When arylaminomethyl( ethyl)pyrazolopyrimidine was treated with formaline (30%) solution in ethanol, underwent Mannich reaction to afford imidazopyrazolopyrimidines (5a-e) and pyrazolopyrimidopyrimidines (8a-e). Chloromethylpyrimidine derivative 3 was converted into the corresponding mercaptomethylpyrazolopyrimidene 9, Which cyclized using bromomalononitrile or phenacyl bromide into pyrazolopyrimidothiazine 11,12.

Apparent Digestibility of Amino Acids, Energy and Proximate Nutrients in Grain Sources and Tapioca for Young Pigs

  • Cho, S.B.;Kim, J.H.;Yang, J.S.;Moon, H.K.;Chae, B.J.;Han, In K.
    • Asian-Australasian Journal of Animal Sciences
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    • v.10 no.6
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    • pp.635-642
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    • 1997
  • This experiment was conducted to determine apparent ileal and fecal digestibilities of some grains for young pigs (15.6 kg BW). Ileal and fecal digestibility of corn, milo, wheat, barley, rice and tapioca were measured with pigs fitted with simple ileal T-cannula. Rice was the highest (p < 0.05) and tapioca was the lowest (p < 0.05) in the digestibilities of gross energy. For the crude protein digestibilities, rice, barley and wheat were higher (p < 0.05) than corn, milo and tapioca. The average ileal digestibilities of essential amino acids (AAs) were 89.9, 85.8, 81.5, 80.9, 80.2 and 76.3% for those fed rice, barley, milo, wheat, corn and tapioca diets, respectively. Regardless of the dietary carbohydrate sources, among the dispensable amino acids, glycine had lowest digestibility except for barley and milo. The apparent ileal digestibility of lysine and methionine were 90.7, 94.0% in rice, 88.3, 86.5% in barley and 86.3, 82.3% in wheat. The apparent fecal digestibility of average essential AAs were 90.8, 89.9, 87.7, 85.1, 82.5 and 77.9% in pigs fed the rice, barley, wheat, corn, milo and tapioca diets, respectively. The fecal digestibilities of essential AAs and nonessential AAs, in general, were higher than the ileal digestibilities, which indicating a loss of nitrogenous components in the cecum and colon. For all AAs, differences between ileal and fecal amino acid digestibilities ranged from 0.0 (valine) to 5.8 (threonine) in rice, 0.1 (arginine) to 14.5 (glycine) in barley, 2.8 (lysine) to 12.4 (glycine) in wheat, 1.0 (isoleucine) to 12.9 (glycine) in corn, 0.2 (serine, glutamic acid) to 6.5 (methionine) in milo and 0.5 (valine) to 22.1 (glycine) percentage units in tapioca diets. In conclusion, whether it is ileal or fecal, rice and barley appeared to be excellent alternative carbohydrate sources for young pigs in terms of AAs digestibility. However, energy value and cost for each grain should be considered when formulating diets.

SCP Production from Mandarin Orange Peel Press Liquor (감귤과피 압착액을 기질로 한 SCP 생산)

  • 강신권;성낙계
    • Microbiology and Biotechnology Letters
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    • v.17 no.6
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    • pp.556-562
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    • 1989
  • The bioconversion of mandarin orange peel press liquor to single cell protein (SCP) by two yeast strains, F-60, and C-7, which were isolated from mandarin orange peel was carried out and compared with that of using Candida utilis IFO 0598. Experiments were directed toward the high yield of biomass and high protein in cultures of the strains mentioned above. Candida utilis IFO 0598, F-60 and C-7 strains were cultivated at 3$0^{\circ}C$, pH 5.2 for 3 days in shaking flasks. The effects of some nutrients on cell growth were studied. Cell mass and protein content per cell mass were increased by addition of urea 1%, KH$_2$PO$_4$ 0.1% and MgSO$_4$ㆍ7$H_2O$ 0.05%, When the F-60 strain cultured under the optimal conditions, cell mass, growth yield and protein content were 41.2g/l, 53.9%, 59.7%, respectively. Cell mass was also increased up to 15% by modifying the fermentation condition on the bench type 20l jar fermentor. Crude fat content (10.3%) of dried C-7 cell was higher than those of C. utilis and F-60, 4.9% and 5.6% respectively. Total protein content of the F-60 strain was 59.7% per dry weight. And we compared their amino acid compositions with that of FAO provisional pattern. In the case of the F-60 strains, amino acid contents such as lysine, leucine and isoleucine were much higher than those of methionine, cystine and tryptophan.

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