• Title/Summary/Keyword: Sulfanilamide

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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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Degradation of Sulfonamide Antibiotic Substances by Ozonation: An Experimental and Computational Approach (설폰아미드계 항생물질의 오존산화분해에 대한 계산화학적 해석 및 실험적 검증)

  • Won, Jung Sik;Lim, Dong Hee;Seo, Gyu Tae
    • Journal of Korean Society of Environmental Engineers
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    • v.36 no.6
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    • pp.442-450
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    • 2014
  • Concern has grown over a presence of micropollutants in natural water since sulfonamide antibiotic substances such as sulfamethazine, sulfamethoxazole, sulfathiazole have been frequently detected in Nakdong River, Korea. The current work investigates the degradation of the three sulfonamide substances by using quantum chemistry calculations of density functional theory (DFT) and experimental measurement techniques of Fourier transform infrared spectroscopy (FT-IR) and ultraviolet-visible spectrophotometer (UV-VIS). DFT calculations demonstrate that the lowest energy gap between the highest occupied molecular orbital (HOMO) and the lowest unoccupied molecular orbitals (LUMO) lies in sulfanilamide functional group of sulfonamide, implying that the sulfanilamide functional group would be the most active site for ozone oxidation. Also, UV-VIS spectra and FT-IR analysis reveal that 260 nm band originated from sulfanilamide group was absent after ozone oxidation, indicating that a functional group of amine (N-H) was removed from sulfanilamide. Both theoretical and experimental observations agree well with each other, demonstrating the DFT calculation tool can be an alternative tool for the prediction of chemical reactions in purification treatment processes.

The Effect on the Dissolution Rate of Sulfanilamide Granules Coated with a Polyelectrolyte Complex of Sodium Tripolyphosphate-Chitosan (Sodium Tripolyphosphate-Chitosan의 Polyelectrolyte Complex Coating이 Sulfanilamide 과립의 용출에 미치는 영향)

  • Ku, Young-Soon;Kim, Ja-Young;Kim, Kil-Soo
    • YAKHAK HOEJI
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    • v.33 no.6
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    • pp.324-332
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    • 1989
  • Drug release from sulfanilamide granules coated with a polyelectrlyte complex of sodium tripolyphosphate and chitosan was studied. The coating film thickness increased with increasing concentration of chitosan in the coating solution and the drug release rates of the coated granules were significantly reduced comparing with those of the uncoated granules. $T_{50%}$ of the uncoated granules was 6 minutes, but those of the granules coated with chitosan-sodium tripolyphosphate from 0.5, 0.7, and 0.9% (w/v) chitosan-HCl solution were 27, 135, and 180 minutes, respectively in distilled water. In dissolution medium at pH 6.8, $T_{50%}$ of the uncoated granules was 4 minutes, but those of the granules coated with chitosan-sodium tripolyphosphate from 0.5, 0.7, and 0.9(w/v)% chitosan-HCl solution, were 32, 135, and 160 minutes, respectively.

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The Influence of the Local Anesthetics on the Absorption of Sulfanilamide through the Rectum (국소마취제(局所麻醉劑)가 Sulfanilamide의 직장내(直腸內) 흡수(吸收)에 미치는 영향)

  • Ha, Chun-Ja;Lee, Jin-Hwan;Choi, Jun-Shik
    • The Korean Journal of Pharmacology
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    • v.9 no.1
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    • pp.53-58
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    • 1973
  • Author attempts to determine the absorption of the sulfanilamide by the various suppositorial bases contained the local anesthetics through the rectum of the rabbit. The types of bases examined are four of lipophillic, hydrophillic and emulsion types such as oil in water and water in oil, otherwise the local anesthetics are procaine and lidocaine each other 2 and 20 percent in a suppository. The results are as follows; 1. The absorption of sulfanilamide is higher when they are combined with the local anesthetics than when single drugs of them are used. 2. The promotion of absorption by the local anesthetics, both the procaine and lidocaine, are higher when they are used 20 percent than 2 percent as the concentration. 3. In excellency of the suppositorial base, the order of the blood level is polyethylene glycol, oil in water, water in oil as emulson type and cacao butter.

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Studies on the Synthesis and Antibacterial Activity of 5-Nitro-2 -furfurylidene Sulfanilamides (5-Nitro-2-furfurylidend sulfanilamide류의 합성과 항균작용에 관한 연구)

  • 박정섭
    • Korean Journal of Microbiology
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    • v.12 no.2
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    • pp.77-84
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    • 1974
  • In order to study 5-nitro-2-furaldehyde derivatives having more effective antibacterial activity, four new $N^4$-(5-nitro-2-furfurylidene)-$N^1$-substituted sulfanilamides$N^1$-3,4-dimethyl-5-isoxazoyl-$N^4$-5-nitro-2-furfurylidene sulfanilamide, $N^1$-4,6-dimethyl-2-pyrimidyl-$N^4$-5-isoxazoyl-$N^4$-5-nitro-2-furfurylidene sulfanilamide, $N^1$-6-methoxy-3-pyridazinyl-$N^4$-5-nitro-2-furaldehyde with sulfa drugs such as sulfisoxazole, sulfamethazine, sulfamethoxypyridazine, and sulfadimethoxine. All compounds were tested for antibacterial activity in vitro on the following micro-organisms : Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Proteus vulgaris. Each compound exhibited a fair bacteriostatic activity against each microorganism. Above all, sulfisoxazole derivatives showed higher activity than the others. Each compound was most active against Staphylococcus aureus, whereas least active against proteus vulgaris.

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Research of Thermal Properties for Liquid Crystalline Epoxy Composites with Tin Oxide Filler (산화주석을 함유한 열경화성 액정 에폭시의 열적 특성에 관한 연구)

  • Hyun, Ha Nuel;Cho, Seung Hyun
    • Composites Research
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    • v.33 no.1
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    • pp.25-29
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    • 2020
  • A liquid crystalline thermosetting-epoxy-based composite was fabricated using diglycidyl ether of 4,4'-biphenol, tin(IV) oxide as a filler, and sulfanilamide as a curing agent. To investigate the thermal behavior, Thermogravimetric Analysis and Laser Flash Apparatus were performed using 3.0-7.0 wt% Tin(IV) oxide. The result showed that the activation energy and thermal conductivity were proportional to the amount of added filler.

Studies on Analysis of Food Additives- (I) Studies on the Determination of Nitrite in Foods (식품첨가물의 분석에 관한 연구 - (I) 아질산근 정량법에 관한 검토)

  • 천석조;천석조;송인상;노정배
    • Journal of Food Hygiene and Safety
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    • v.3 no.2
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    • pp.53-58
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    • 1988
  • This study was carried out to discuss a colorimetric method for the determination of nitrite in meat products issued by the Ministry of Health and Social Affaires of Korea (1985). 1) The recovery rates of nitrite of test solution extracted in the room temperature were higher than those obtained by the heating extraction. 2) In the room temperature, samples prepared with the sUce were more effective than the blendina method and the distlled water as extractina solvent for nitrite was more effective tban tbe phospbate buffer solution. 3) The extracting time showed that thirty minutes were enough to extract nitrite and the diazotizingcoupling reagents, 30% of sulfanilamide and N-l-naphthylethyienediamine were better than others. 4) The nitrite in a test soiution greatly decreased when the solution was distilled. In this case, the test solution should be used as a control. 5) Ten minutes were enough to couple nitrite.

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Production of L-Tryptophan by Auxotrophs Derived from Analogue- resistant Mutants of Escherichia coli (영양요구성 대장균 변이주를 이용한 L-트립토판 생산)

  • Lee, In-Young;Kim, Jae-Hi;Kwak, Moo-Young;Lee, Hosull;Lee, Sun-Bok
    • Microbiology and Biotechnology Letters
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    • v.16 no.5
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    • pp.407-412
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    • 1988
  • In order to increase the tryptophan productivity of E. coli SB1007, a mutant resistant to sulfanilamide was isolated and then a tyrosine auxotroph TY-90 was derived from the sulfanilamide-resistant mutant SA3-39-16. In the test-tube culture a quantitative amount of tryptophan was accumulated in strain TY-90 but in a jar fermentor culture the productivity was lower as compared to the level obtained by the parent strain. From the double auxotrophic mutant SB2756, a revertant resistant to 2, 000$\mu\textrm{g}$/$m\ell$ of $\beta$-thienylalanine, TA 40-10, was selected and then phenylalanine auxotrophs were derived from the revertant strain TA-40-10. One of the phenylalanine auxotrophs, TP-4, accumulated 3.7g/$\ell$ of L-tryptophan after 71-hr cultivation in a jar fermentor experiment.

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Characterization of Antibacterial activity and Synthesis of Sulfanilamide Polymer using Crosslinking Agent (가교제를 이용한 Sulfanilamide 중합체의 합성과 항균특성)

  • Kim, Jong-Woan;Yoon, Chul-Hun;Hwang, Sung-Kwy;Kong, Seung-Dae;Lee, Han-Seab
    • Journal of the Korean Applied Science and Technology
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    • v.17 no.1
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    • pp.37-42
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    • 2000
  • Drug delivery system(DDS) have been actively studied for the past twenty years. Dual action agents are unique chemical entities comprised of two different types of antibacterial compounds covalently linked together in a single molecule in such a way that both components are able to exert their bactericidal properties. In spite of the advent of the antibacterial agent the sulfa agents are the most widely used antibacterial agent today. In this study, new antibacterials derivative was synthesized using glutaraldehyde such as crosslinking agent for the purpose of dual-action as DDS study. Antibacterial activity of these new synthetic derivative between their structures and activities were examined by disc diffusion method. As a result, new synthetic derivative exhibited the broad antibacterial activities against Gram(+) and Gram(-) bacilli. Especially, the antibacterial effect of new synthetic derivative against Gram negative(Esherichia. coli) was much stronger than that against Gram positive.

Effect of Polysorbate 80 on the Dissolution of Sulfanilamide and Sulfacetamide Granules (Polysorbate 80이 Sulfanilamide및 Sulfacetamide 과립의 용출에 미치는 영향)

  • 구영순;이정순
    • YAKHAK HOEJI
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    • v.31 no.3
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    • pp.189-196
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    • 1987
  • This study was carried out to investigate the effect of surfactant on the dissolution of relatively hydrophilic drugs, such as sulfanilamide (SF) and sulfacetamide (SFA) granules prepared by wet granulation. The additive incorporated in the granules is starch or microcrystalline cellulose(MCC) as an excipient, PVP as a binder, and polysorbate 80 (P-80) as a surfactant. The dissolution characteristics of SF and SFA granules in distilled water were as follows: The values of T$_{75%}$ were 4.60 and 2.50min, respectively for SF and SFA granules. Incorporation of 0.1% P-80 in SF granule ratarded the dissolution of SF as compared with control, but addition of 0.1% P-80 to SFA granule improved the dissolution of SFA in comparison with control. In SF and SFA granules formulated with either starch or PVP, the release of the drug was increased as compared with control. In SF granule, the dissolution of the drug was further reduced by the inclusion of P-80 in the granule containing starch or PVP. Incorporation of P-80 in SFA granule with starch or PVP affected little on the dissolution of the drug. Addition of a nonswelling excipient, MCC decreased the dissolution rate of SF and SFA granules. as compared with each control. The presence of P-80 in these granules made the dissolution rate slower in comparison with the granules containing only MCC.

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