• Archives of Pharmacal Research
• /
• v.14 no.4
• /
• pp.319-324
• /
• 1991

2,6-Dimethyl-4-(3'-nitrophenyl)-3-methoxylaminocarbonyl-1,4-dihydropyridine-5-carboxylic acid methylester, 3b reacted with 2-cyanoethanol or benzylalcohol to give the corresponding cyanoethylurethane compound 6c in 40.6% yield and benzylurethane compound 6d in 32% yield. The cyanoethylurethane 6c was hydrolized in ethanolic NaOH to give 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3-amino-5-carboxylic acid 5-methyl ester. HCl 8 in 64.8% yield. Another acid hydrolysis of benzylurethane 6d gave 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3-amino-5-carboxylic acid 5-methylester. HBr 11 in 54.7% yield.

• Journal of the Korean Applied Science and Technology
• /
• v.15 no.1
• /
• pp.63-78
• /
• 1998

A series of long chain N-acyl amino acid type anionic surfactants were prepared by treating fatty acid chlorides with three kinds of amino acids, that is, sodium N-acyl-sarcosinates, sodium N-acyl-N-methyl-${\beta}$-alaninates and sodium N-acyl-N-methyl-taurates in an alkaline solution. All prepared biodegradable surfactants were purified by thin layer chromatography and column chromatography, and identified their structures by spectral analysis.

• Bulletin of the Korean Chemical Society
• /
• v.35 no.4
• /
• pp.1087-1090
• /
• 2014

A simple and general method that selectively introduces metal binding sites into a protein can greatly increase the ability to design and biosynthesize artificial metalloproteins. Here, we report the incorporation of a phenanthroline-containing amino acid (Phen-Ala) into proteins in Escherichia coli by using the $tRNA{^{Tyr}}_{CUA}$ and tyrosyl aminoacyl-tRNA synthetase pair (BpyRS) from Methanococcus jannaschii, which was originally developed for a bipyridine-containing amino acid (Bpy-Ala). The incorporation efficiency of BpyRS for Phen-Ala was comparable to that for Bpy-Ala. Because of its high metal-binding ability and characteristic spectral properties, Phen-Ala can be a useful alternative to the existing metal-chelating amino acids for the design and synthesis of artificial metalloproteins.

• Bulletin of the Korean Chemical Society
• /
• v.17 no.4
• /
• pp.314-321
• /
• 1996

Isoxazolidine derivatives 7 and 8 were synthesized from N-benzyl-C-(2-benzyloxyethyl)nitrones by 1,3-dipolar cycloaddition with ethyl crotonate. The isoxazolidine derivatives were converted to β-amino acid esters 9a and 9b by reduction with zinc in acetic acid. The β-amino acid esters were reacted with methylmagnesium bromide to give the 2-azetidinones (13a, 13b). The benzyl group of 2-azetidinones were removed by Birch reduction. The products were oxidized with PDC to give 3-[1-(t-butyldimethylsilyloxy)ethyl]-4-carboxymethyl-2-azetidinone derivatives (2a, 2c).

• Asian-Australasian Journal of Animal Sciences
• /
• v.13 no.3
• /
• pp.300-306
• /
• 2000

This experiment was carried out to determine the contributions of acetate, glucose, amino acids and amino acid metabolites as carbon precursors for the incorporation of radioisotope, in intramuscular and subcutaneous adipose tissue and the effects of insulin on lipogenesis and adrenergic agent, norepinephrine on lipolysis in both tissues. The rate of incorporation of $C^{14}$ labelled acetate, glucose, leucine, isoleucine and ${\alpha}$-ketoisocaproic acid into adipose tissue has been measured in subcutaneous and intramuscular adipose tissues. The rate of incorporation was greater (p<0.05) from acetate than glucose in both subcutaneous and intramuscular adipose tissue and the rate of incorporation of carbon precursors into adipose tissues was greater in subcutaneous than in intramuscular adipose tissues. In comparison of amino acids, the rate was highest (p<0.05) with leucine followed by isoleucine and ${\alpha}$-ketoisocaproic acid in subcutaneous adipose tissue, in which there were no differences. Also, in intramuscular tissue, leucine was highest (p<0.05), and the rate of incorporation decreased in the same order. The rates of carbon precursor incorporation appeared to be higher in subcutaneous than in intramuscular tissue. For incorporation of radio-labelled acetate and glucose into intramuscular adipose tissue. preincubated for 48 hrs with insulin and IGF-1, insulin was the most effective to stimulate the incorporation of precursors in both substrates but there was no difference between insulin and IGF-1 in glucose incorporation. For glyceride-fatty acid synthesis, acetate was significantly (p<0.05) greater than glucose in both subcutaneous and intramuscular adipose tissue, and glyceride-glycerol synthesis was greater (p<0.05) for glucose than acetate in both adipose tissues. The rates of lipogenesis from both precursors were slightly greater in subcutaneous than intramuscular adipose tissue. There was significant (p<0.05) site effect in insulin treatment for glyceride-fatty acid synthesis. But there were no significance in control and norepinephrine. For glyceride-glycerol synthesis, there was no site effect caused by hormonal treatment. Insulin was the most effective (p<0.05) in glyceride fatty acid synthesis, while norepinephrine was the same as control. Compared with control, glyceride-glycerol synthesis from acetate in insulin treatment was significantly (p<0.05) low in subcutaneous, but high in intramuscular tissue. At the same time, in both tissues, it was lower in norepinephrine treatment than in control. Glyceride-glycerol synthesis from glucose was highest (p<0.05) in norepinephrine treatment followed by insulin although there was no significance between insulin and control. Lipolysis was not affected by insulin but was increased by norepinephrine when added to adipose tissue incubations in vitro. Rates of basal lipolysis were greater in subcutaneous adipose tissue than in intramuscular adipose tissue.

• Archives of Pharmacal Research
• /
• v.26 no.6
• /
• pp.441-445
• /
• 2003

New sulfonated amino ribofuranans were synthesized to elucidate the relationship between structure and specific biological activities such as anti-HIV and blood anticoagulant activities. The synthesis was performed by sulfonation of copolymers having various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranosidic unit. The sulfonation with piperidine N-sulfonic acid produced the sulfonated amino ribofuranans in high yield. The anti-HIV activity of sulfonated 3-amino-3-deoxy-(1$\rightarrow5)-\alpha$-D-ribofuranan showed more potent by increasing the degree of sulfonation and the average molecular weights. This activity was almost equal to the activities of sulfonated ribofuranans and ribopyranans reported before in spite of low molecular weight. The blood anticoagulant activities was observed at 36-48 mg/units, more potent than standard dextran sulfonate, 22.7 mg/units. In addition, the blood anticoagulant activities of sulfamide-copolysaccharide consisting various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranan units were potentiated by increasing sulfonated amino-ribofuranan units from 13 to 21 mg/units.

• YAKHAK HOEJI
• /
• v.30 no.6
• /
• pp.294-300
• /
• 1986

New antibiotics having moieties of penicillanic acid, cephalosporanic acid and ampicillin on both ends of the central polyalkylene were synthesized by reacting 6-aminopenicillanic acid (6-APAl), 7-amino cephalosporanic acid (7-ACA) and ampicillin with hexamethylene diisocyanate and sebacoyl chloride, respecetively. Antibiacterial activities of the compounds were also investigated.

• Journal of the Korean Chemical Society
• /
• v.54 no.5
• /
• pp.506-514
• /
• 2010

A new series of ligands N-[(benzoylamino)-thioxomethyl]-amino acid (HL) were synthesized by reaction of benzoylisothiocyanate with various amino acids namely aspartic acid [BATA] (1), glutamic acid [BATG] (2), methionine [BATM] (3), leucine [BATL] (4), and tryptophan [BATT] (5). The ligands were characterized by elemental analysis, IR and NMR spectra. Some transition metal complexes ($ML_2$) for these ligands (6-8) were prepared; [M=Cu(II), Co(II), or Ni(II)], and characterized by elemental analysis, IR and $^1H$ NMR spectra. Antibacterial study showed that all the ligands have no antibacterial activity, whereas ($ML_2$) complexes; [M = Cu(II), Co(II), or Ni(II)] have antibacterial activity towards (Gram -ive) Escherichia (NCTC5933) and (Gram +ive) Staphylococcus (NCTC6571) and have no toxicity on (BALB/C) Albino mice.

• YAKHAK HOEJI
• /
• v.3 no.1
• /
• pp.4-9
• /
• 1957

Effects of antibioties on micro-organism have been reported by many scientists, such as Krampitz and Werkman, Fisher, Gale and Rodwell, Klimick Cavalito and Bailey, Umbreit, etc. On the mechanism by which penicillin act, Fisher(1947), Platt(1947), and Cavallito, considered that penicillin might act on bacteria by inhibiting with the normal function of SH-group of glutathione in the metabolism of the cell. Resenbrance of penicillin to gultathione in structure and the inactivation of penicillin by cysteine make us approve of the above inhibiting theory of SH-group. Galland (1947) and Schmidt (1947) reported that penicillin inhibited the activity of ribonuclease, Phosphatase, and mononucleotidase. Gale (1948) discovered that the gram positive bacteria had lost the power to uptake glutamic acid by ribonucleic acid in the medium contained penicillin: growth of gram positive organism was inhibited by the results that penicillin inhibited the uptake of amino acid byribonucleic acid, acting on ribonucleic acid of gram positive bacteria. Hotchkiss (1950) cultured S. aureus in the medium contained glucose and amino acids, and studied the effect of penicillin on protein synthesis. Peptide formation in living cells was inhibited by penicillin, while amono acid was utilized as before the addition of penicillin. On the otherhand, Binkley (1951) found penicillin interfered hydrolase of glutath one, and Hans (1950) reported penicillin inhibited the transpeptidation. On the machanism by which streptomycin acts. Cohen (1947) reported steptomycin made a irreversible complex with desoxyribonucleic acid, by the fact that desoxyribonucleic acid formed the precipitates with diguanide group of steptomycin. Zeller (1951) reported, on the other hand, streptomycin inhibited diamine oxidease. Geiger (1947) and Umbreit (1949) reported that steptomycin inhibited condensation of oxaloacetate and pyruvate in E. Coli and Oginsky et al (1949) reported steptomycin inhibited oxaloacetate-pyruvate reaction in Kreb's cycle. On the mechanism by which terramycin acts, Hahn & Wisseman (1951) reported that the formation of adaptive enzyme was inhibited by terramycin in E. Coli cultivated in the medium contained loctose, and that the protein synthesis was inhibited by terramycin. However, effects of antibiotics on amino acid metabolism have not been discussed much in spite of its important role in living cells. Especislly, effects of anitibiotics on higher plants have scarcely been reported. Here, to prove the effect of antibiotics on higher plants, and the mechanism by which, through amino acid metabolism, they promote or inhibit growth of plants, amino acids in bean plants treated with penicillin, streptomycin, and terramycin were analyzed by paper chromatography. And to clarify the antagonis of cysteine (as SH-group) against penicillin, through amino acid metabolism, amino acids in bean plants treated with cystene and penicillin, at the same time, were also analyzed.

• Asian-Australasian Journal of Animal Sciences
• /
• v.13 no.4
• /
• pp.543-560
• /
• 2000

The present paper gives a general overview on amino acid nutrition mainly focused on the concept of ideal protein and amino acid requirements in swine and poultry. Also, the nutritional, economic and environmental roles of synthetic amino acids are presented. A special emphasis has been given to the protein sparing effect by the supplementation of synthetic amino acids into diet and to the effect of this supplementation on growth performance and reduction of environmental pollutants in swine and poultry manure. It is concluded that the supplementation of limited amounts of synthetic amino acids (0.1 to 0.3%) to diets for swine and poultry could spare 2 to 3 percentage units of dietary protein and substantially reduce nutrient excretion, especially nitrogen. Immunocompetency as affected by amino acid nutrition is also introduced and the importance of threonine for the synthesis of immunoproteins in colostrum and milk to maintain piglets' health and intestinal integrity has been emphasized. Finally, some speculation on the future of global amino acids market is presented in conclusion.