• Title/Summary/Keyword: antibacterial action.

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Synthesis and Biological Activities of Carbamate Derivative (Carbamate 화합물의 합성 및 위생학적 연구)

  • 강회양
    • Journal of Environmental Health Sciences
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    • v.22 no.2
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    • pp.19-24
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    • 1996
  • Carbamates are generally used as insecticide, thus 5.7-dichloro-8~hydroxyquinolinyl- N-ethylcarbamate was newly synthesized. Its physical properties were determined and chemical structure was identified by means of I.R., nmr in addition to elemental analysis. The yield of addition, using triethylamine as catalyst, 5.7-dichloro-8-hydroxyquinoline and isocyanate was better than that of condensation of 5.7-dichloro-8-hydroxyquinoline with carbamoylchloride. The effct of the compound on rabbit's ileum, and antibacterial activity against Staphylococcus aureus, Salmonella typhi, Echerichia coli, and Pseudomonas aeruginosa were examined. The present organic synthesized compound showed the bacteriostatic action on salmonella typhi, escherichia coli, and pseudomonas aeruginosa, but no otherwise effect of contraction of rabbit's ileum in the concentration of $250 \mu g/ml$.

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Studies on the synthesis and antibacterial action of $N^4$-furoylsulfonamides ($N^4$-furoylsulfanamide류의 합성및 항균작용에 관한 연구)

  • 고현기
    • YAKHAK HOEJI
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    • v.13 no.2_3
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    • pp.62-66
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    • 1969
  • Ten new N$^{4}$-furoylsulfonamides were synthesized such as N$^{4}$-furoyl-N$^{1}$-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide (I), N$^{4}$-furoylsulfanilamide (II), N$^{4}$-furoyl-N$^{1}$-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide (III), N$^{4}$-furoyl-N$^{1}$-(4-methyl-2-pyrimidinyl) sulfanilamide (IV), N$^{4}$-furoyl-N$^{1}$-(6-methoxy-3-pyridazinyl) sulfanilamide (V), N$^{4}$-furoyl-N$^{1}$-2-pyrimidinylsulfanilamide (VI), N$^{4}$-furoyl-N$^{1}$-(3,4-dimethyl-5-isoxazolyl) sulfanilamide (VII), N$^{4}$-furoyl-N$^{1}$-2-thiazoilysulfanilamide (VIII), N$^{4}$-furoyl-N$^{1}$-(5-methoxy-2-pyrimidinyl) sulfanilamide (IX) and N$^{4}$-furoyl-N$^{1}$-(2,6-dimethyl-4-pyrimidinyl) sulfanilamide (X). They were obtained by the action of N$^{1}$-(4,6-dimethyl-2-pyrimidinyl) sulfanilamide, N$^{1}$-(2,6-dimethoxy-4-pyrimidinyl) sulfanilamide, N$^{1}$-(4-methyl-2-pyrimidinyl) sulfanilamide, N$^{1}$-(6-methoxy-3-pyridazinyl) sulfanilamide, N-2-pyrimidinyl sulfanilamide, N$^{1}$-(3,4-dimethyl-5-isoxazolyl) sulfanilamide, N$^{1}$-2-(thiazolysulfanilamide), N$^{1}$-(5-methoxy-2-pyrimidinyl) sulfanilamide and N$^{1}$-(2,6-dimethyl-4-pyrimidinyl) sulfanilamide with furoyl chloride in 4% NaOH solution. Of the above ten compounds, N$^{4}$-furoylsulfathiazole exhibited a good antibacterial action against Staphylococeus aureus and Escherichia coli.

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Screening of Lactobacilli Derived from Fermented Foods and Partial Characterization of Lactobacillus casei OSY-LB6A for Its Antibacterial Activity against Foodborne Pathogens

  • Chung, Hyun-Jung;Yousef, Ahmed E.
    • Preventive Nutrition and Food Science
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    • v.14 no.2
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    • pp.162-167
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    • 2009
  • Various fermented foods were screened in search of food-grade bacteria that produce bacteriocins active against Gram-negative pathogens. An isolate from a mold-ripened cheese presented antibacterial activity against Gram-positive and Gram-negative bacteria. The most active isolate was identified as Lactobacillus casei by a biochemical method, ribotyping, and membrane lipid analysis, and was designated as OSY-LB6A. The cell extracts of the isolate showed inhibition against Escherichia coli p220, E. coli O157, Salmonella enerica serovar Enteritidis, Salmonella Typhimurium, and Listeria monocytogenes. The antibacterial nature of the cell extract from the isolate was confirmed by eliminating the inhibitory effects of acid, hydrogen peroxide, and lytic bacteriophages. The culture supernatant and cell extract retained antibacterial activity after heating at $60{\sim}100^{\circ}C$ for $10{\sim}20$ min. The activity of the cell extract from Lb. casei was eliminated by pronase and lipase. Finally, the cell extract showed a bactericidal mode of action against E. coli in phosphate buffer solution, but it was bacteriostatic in broth medium and food extracts.

Different modes of antibiotic action of homodimeric and monomeric bactenecin, a cathelicidin-derived antibacterial peptide

  • Lee, Ju-Yeon;Yang, Sung-Tae;Kim, Hyo-Jeong;Lee, Seung-Kyu;Jung, Hyun-Ho;Shin, Song-Yub;Kim, Jae-Il
    • BMB Reports
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    • v.42 no.9
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    • pp.586-592
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    • 2009
  • The bactenecin is an antibacterial peptide with an intramolecular disulfide bond. We recently found that homodimeric bactenecin exhibits more potent antibacterial activity than the monomeric form and retains its activity at physiological conditions. Here we assess the difference in the modes of antibiotic action of homodimeric and monomeric bactenecins. Both monomeric and dimeric bactenecins almost completely killed both Staphylococcus aureus and E. coli within 10-30 min at concentrations of $8-16\;{\mu}M$. However, exposure to liposomes elicited an increase in the fluorescence quantum yield from a tryptophan-containing monomeric analog, while the homodimeric analog showed a significant reduction in fluorescence intensity. Moreover, unlike the monomer, the homodimer displayed apparent membrane-lytic activity enabling release of various sized dyes from liposomes, and rapidly and fully depolarized the S. aureus membrane. Together, our results suggest that homodimeric bactenecin forms pores in the bacterial membrane, while monomeric one penetrates through the membrane to target intracellular molecules/organelles.

Antibacterial Activities of Nonactin from streptomyces viridochromogenes JM-4151

  • Lee, Jin-Man;Lee, Dong-Sun;Lee, Sang-Han;Hong, Soon-Duck;Kim, Jong-Guk
    • Journal of Life Science
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    • v.10 no.1
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    • pp.45-47
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    • 2000
  • Nonactin, known as an ionophore antibiotic, was antagonized by the actibity of quercetin, an oxygen radical scavenger. This compound generated superoxide radicals in Bacillus subtilis lysates. A recombination-deficient mutant strain of B. subtilis was more sensitive than a wild strain, and this hypersensitivity was reduced in the presence of dithiothreitol as an antioxidant. These results suggest that superoxide radical is important in the antibacterial action of this agent.

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CPC-222, A New Fluoroquinolone

  • Lee, Younha
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.12-12
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    • 1997
  • CFC-222 is a novel fluoroqinolone antibacterial agent synthesized and under development by the Cheil Jedang Corporation, Korea. CFC-222 exerts the antibacterial activity by inhibition of bacterial DNA gyrase leading to bactericidal action. In in vitro and in vivo preclinical testing, CFC-222 has been shown to possess a broad spectrum of antibacterial activity. In particular CFC-222 is very potent against Gram-positive bacteria such as Staphylococcus spp., Streptocuccus spp. (in particular penicillin G-resistant and -susceptible S. pneumoniae) and Enterococcus spp. when compared to other quinolones (ciprofloxacin, ofloxacin or lomefloxacin). CFC-222 also showed potent activity against the methicillin resistant clinical isolates of S. aureus (MRSA). Against Gram-negative bacteria (E. coli, Pseudomonas and Sarcina) the activity of CFC-222 was slightly weaker than that of ciprofloxacin, but was more potent than that of ofloxacin or lomefloxacin. In urinary systemic infections caused by both Gram-positive and -negative bacteria, CFC-222 demonstrated a potent therapeutic efficacy in particular against Cram-positive bacteria S. aureus, S. pyrogen 203 and S. pneumonia TypeIII.

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Synthesis of Hybrid Bivalent Ligand Quinolone Derivatives (혼성 Bivalent Ligand 퀴놀론 유도체의 합성)

  • Lee, Sang-Pil;Im, Chae-Uk;Kim, Dong-Soon;Yim, Chul-Bu
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.664-672
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    • 1994
  • Eighteen new hybrid bivalent ligand quinolones that contain two different type of pharmacophores in a single molecule were prepared and evaluated for in viかo antibacterial activity. Hybrid bivalent ligands p-nitrobenzyloxycarbonyl quinolones were prepared by the treatment of active esters of succinyl fluoroquinolones with 1,7-disubstituted fluoroquinolone carboxylic acids in DMF. Eighteen final quinolone carboxylic acids were obtained by the reduction of compounds $25{\sim}42$ with hydrogen in the presence of 10% Pd-C. Among these derivatives, compound[56] showed the most potent antibacterial activity against a wide range of microoranisms.

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Inhibitory Effects of Synthetic Peptides Containing Bovine Lactoferrin C-lobe Sequence on Bacterial Growth

  • Kim, Woan-Sub;Ohashi, Midori;Shimazaki, Kei-ichi
    • Food Science of Animal Resources
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    • v.36 no.4
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    • pp.452-457
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    • 2016
  • Lactoferrin is a glycoprotein with various biological effects, with antibacterial activity being one of the first effects reported. This glycoprotein suppresses bacterial growth through bacteriostatic or bactericidal action. It also stimulates the growth of certain kinds of bacteria such as lactic acid bacteria and bifidobacteria. In this study, Asn-Leu-Asn-Arg was selected and chemically synthesized based on the partial sequences of bovine lactoferrin tryptic fragments. Synthetic Asn-Leu-Asn-Arg suppressed the growth of Pseudomonas fluorescens, P. syringae and Escherichia coli. P. fluorescens is a major psychrotrophic bacteria found in raw and pasteurized milk, which decreases milk quality. P. syringae is a harmful infectious bacterium that damages plants. However, synthetic Asn-Leu-Asn-Arg did not inhibit the growth of Lactobacillus acidophilus. It is expected that this synthetic peptide would be the first peptide sequence from the bovine lactoferrin C-lobe that shows antibacterial activity.

Studies on the Efficacy of Combined Preparations of Crude Drug (II) -The Effect of ‘Kamisamhwang-Tang’ on Cardiovascular System and Antibacterial Activities- (생약복합제제(生藥複合製劑)의 약효연구(藥效硏究) (제2보)(第2報) -가미삼황탕(加味三黃湯)이 순환기계(循環器系) 및 항균작용(抗菌作用)에 대(對)하여-)

  • Hong, N.D.;Kim, J.W.;Song, I.B.;Kim, N.J.
    • Korean Journal of Pharmacognosy
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    • v.12 no.4
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    • pp.190-194
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    • 1981
  • It was prevously shown that 'Kamisamhwang-Tang' had been examined for effects of the anticonvulsion, antipyretic, analgesic and sedative. To investigate the effect on cardiovascular system and antibacterial activities, pharmacological studies have been carried out with each extract. The results of this investigation were summarized as follows: 1) 'Kamisamhwang-Tang' depressed central convulsion induced by strychnine, picrotoxine and caffeine in mice. 2) Antipyretic, analgesic and sedative action were observed. 3) Hypotensive effect was observed in rabbits. 4) Antibacterial activities was observed.

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