• Archives of Pharmacal Research
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• v.15 no.1
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• pp.99-103
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• 1992

Susceptibility of Psudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis to gentimicin and ceforaxime was affected by salicylaye. In presence of salicylaye (15 mM) and gentamicin (1.0 .mu.g/ml), log efficiency of plating (log E. O. P. s) for the tested bacteria were -1.24, -2.17 and -1.66 respectively. The activity of cefotaxime against Bacillus subtilis was reduced (log E. O. P. = 1.33). The highest potentiating effects of salicylaye were shown when using gentamicin against Staphylococcus aureus, cefotaxime against Ps. aeruginosa, log E. O. P.s were -3.0, and -2.4 respectively. On the other hand, no significant effects were detected with cefotaxime against Staphylococcus aureus (log E. O. P. = -0.04). No significant killing was shown in presence of gentamicin or salicylaye alone. There was no significant effect for salicylaye on MICs (By broth dilution) could be observed except in case of gentamicin against Staphyloccus aureus, which was reduced from 0.02 .mu.g/ml to 0.0012 .mu.g/ml. These results raise the concern that high concentrations of salicylaye in patients might interfere with antibiotic therapies.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.106-106
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• 1993

DWC-751은 그람양성 및 음성균주에 대하여 광범위한 항균스펙트럼을 가지는 것으로 나타났다. 그람양성균 S. aureus에 대하여는 cefpirome과 동등하며, cefotaxime 보다 4배, ceftazidime보다 16배 우수하였고 그람음성균에 대하여 DWC-751의 항균력은 cefpirome, cefotaxime보다 2배, ceftazidime보다 4-8배 우수하였다. Ps. aeruginosa에 대한 DWC-751의 항균력은 ceftazidime과 거의 동등한 항균력을 나타내었고, cefpirome보다 2배, cefotaxime보다 4-8배 우수한 항균력을 나타내었다. 임상분리균주 및 ofloxacin 내성균주에 대한 DWC-751의 항균력은 표준균주에 대한 결과와 같이 대조약물보다 우수하였다. 전신감염치료효과에 있어서 Streptococcus pyogenes, Serratia marcescens, Acinetobacter calcoaceticus, Morganella morganii, Proteus mirabilis에 대한 동물실험 결과, ED$_{50}$치에 의한 효능은 cefotaxime 보다 우수하였으며,Enterobacter cloacae, Pseudomonas aeruginosa에 대하여는 ceftazidime과 거의 동등하였다.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.171-171
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• 1994

Cephem ring의 C-7위치에 aminothiazoly lmethoxyimino기를 가진 화합물들이 항균활성을 증가시키고, G(-)균의 외막투과성을 촉진시킬뿐 아니라 광범위항균 spectrum을 갖게 하고 $\beta$-lactamase에 안정하며 PBP(penicillin binding protein)에 대한 결합친화성을 증가시킨다는 보고에 따라 본 저자는 C-7위치에 cefotaxime구조와 같이 aminothiazolylmethoxyimino acetamido moiety를 고정시키고 항균활성을 증가시키기 위하여 약리활성이 기대되는 5-(substituted)-2H-tetrazole유도체들을 합성하여 C-3 위치에 도입시킨 새로운 화합물 7$\beta$-〔(z)-2-(2-aminothiazol-4-yl)-2_(methoxyimino)acetamido〕-3-〔5-(substituted)tetrazol-2-yl〕 methyl-3-cephem-4-carboxylic acid 유도체를 합성하여 B. subtilis ATCC 6633, M. luteus ATCC 1004, E. coli KCTC 1039, E. coli ESS, K. pncumonia KCTC 1560, P. aeruginosa IF0 13130, S. typhimurium KCTC 1925, S. typhimurium SL 1102, 및 C. albicans ATCC 10231 등의 균과 fungus에 대하여 기존의 cefotaxime과 cefazoline을 대조물질로 사용하여 항균력을 비교하였다. 이들 화합물들은 대체적으로 M. luteus ATCC 6633, E. coli ESS, S. typhimurium SL 1102 균에 대해서는 cefotaxime보다 항균력이 우수하였으나 P. aeruginosa IF0 13130에 대해서는 항균력이 저하되었고 cefazolin보다는 대체적으로 항균력이 우수하였다.

• Bulletin of the Korean Chemical Society
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• v.32 no.2
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• pp.407-410
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• 2011

An isolable activated ester, diethyl thiophosphoryl [(Z)-(2-aminothiazol-4-yl)-2-(methoxyimino)acetate (9a, DAMA) was prepared in high purity, which was at least stable for 7 d at $25^{\circ}C$ and 6 months at $5^{\circ}C$. Its reaction with 7-ACA (4) in the presence of tributylamine in i-PrOH provided cefotaxime (1) of high purity in good yield. Preparation of DAMA and its reaction with 7-ACA (4) to 1 was performed in one-pot manner, respectively with minimal unit operations of stirring and filtration.

• Bulletin of the Korean Chemical Society
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• v.8 no.5
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• pp.418-421
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• 1987

Syntheses of cefotaxime analogs with halosubstituted phenyltetrazolthiomethyl at the $C_{3^-}$position are described. Their in vitro potency was established. The compounds exhibited a broad antibacterial spectrum. Some of these compounds showed activity against Gram-positive bacteria superior to the parent cefotaxime. Against Gram-negative bacteria, these compounds are less effective than cefotaxime.

• Archives of Pharmacal Research
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• v.6 no.1
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• pp.55-62
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• 1983

Binding of six cephalosporins (cefotaxime, cefuroxime, cefazoline, cephalothin, cephaloridine, cephacetrile) to bovine serum albumin was studied. Fluorescence probe technique and difference spectrophotometry were employed to evaluate the nature and degree of association of cephalosporin albumin complex. 1-Anilinonaphthalene-8-sulfonate (ANS) was used as the fluorescence probe. 2-(4'-hydroxybenzeneazo) benzoic acid(HBAB) was employed as the UV spectrophotometric probe. Compentitive bindings between cephalosporins and probes were observed. The number of binding sites of bovine serum albumin for each cephalcsporin is 2. Among six cephaloporins, cefotaxime has the highest binding constant followed by cafazoline, cefuroxime, cephalothin, cephaloridine and cephacetrile.

• Horticultural Science & Technology
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• v.19 no.1
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• pp.17-21
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• 2001

To develop a selection system for regenerating plants from transformed tissues, effects of four antibiotics (kanamycin, hygromycin, carbenicillin, cefotaxime) and herbicide (phosphinotricin) on shoot regeneration from cotyledon and hypocotyl explants of Chinese cabbage (Brassica campestris L. ssp. pekinensis) were studied. For cotyledon, shoot induction was not significantly affected by kanamycin at $1mg{\cdot}L^{-1}$, but the number of shoots formed was significantly reduced at $2mg{\cdot}L^{-1}$, and no shoots were regenerated from any explants at $6mg{\cdot}L^{-1}$ or higher. Hypocotyl explants showed similar result as cotyledon. Kanamycin at $7mg{\cdot}L^{-1}$ may be adequate for selecting Chinese cabbage transformants. Hygromycin at $4mg{\cdot}L^{-1}$ or higher completely inhibited the growth and shoot regeneration of Chinese cabbage explants. Therefore, resistance gene to hygromycin may also be used as a selective marker for Chinese cabbage transformation. Carbenicillin and cefotaxime, the cephalosporin type of antibiotics, had little effect on shoot regeneration of Chinese cabbage explants. Since carbenicillin and cefotaxime have low toxicity to Chinese cabbage, they are suitable for use in tissue culture to eliminate Agrobacterium in transformation experiments after co-cultivation. Shoot regeneration from cotyledon and hypocotyl explants was significantly reduced in presence of $1mg{\cdot}L^{-1}$ phosphinotricin (PPT) and completely inhibited by $2mg{\cdot}L^{-1}$ or higher. PPT, same as antibiotics, may also be used to select transformed cells. Since Chinese cabbage is known to be recalcitrant to in vitro shoot regeneration compared to other Brassica species, even though lower levels of selectable markers result in more transformants but simultaneously allow more untransformed escapes to develop, lower levels of antibiotics and herbicides could be successfully used as a selectable marker to reduce selection pressure.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.228.2-229
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• 2003

Investigation of polymorphism has become a requirement in the pharmaceutical industry because the physical properties and bioavailabilities of crystalline drugs depend on their polymorphic form. Two polymorphic modifications and one pseudopolymorphic modification of cefotaxime sodium were prepared by recrystallization in organic solvents under variable conditions. Four polymorphic modifications of cephardine were prepared by recrystallization. Three polymorphic modifications and one pseudopolymorphic modification of ceftriaxone sodium were prepared by recrystallization. (omitted)

• 한국전기화학회:학술대회논문집
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• 2002.04a
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• pp.11-11
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• 2002

• Korean Journal of Medicinal Crop Science
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• v.13 no.1
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• pp.57-62
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• 2005

Salt-tolerant transgenic Panax ginseng plants were produced by introducing the SAL1 geue (3'(2'), 5'-bis-phosphate nucleotidase) that confers tolerance to the salts through Agrobacterium tumefaciens co-cultivation. Cotyledon explants of immature ginseng zygotic embryos cultured on Murashige and Skoog medium lacking growth regulators formed somatic embryos directly with below 10%, but the 74% tranformation rate were observed at the treatment of phytohormone with 1.0 mg/l 2,4-D and 0.5 mg/l kinetin. Somatic embryos were initially cultured on MS medium supplemented with 250 mg/l cefotaxime for 3 weeks and subsequently subcultured five times to a medium containing 100 mg/l kanamycin and 250 mg/l cefotaxime. Upon development into the cotyledonary stage, these somatic embryos were transferred to on the medium containing 50 mg/l kanamycin and 10 mg/l gibberellic acid to induce germination and strong selection. Integration of the transgene into the plants was confirmed by polymerase chain reaction with specific primers. The ginseng transformants with well-developed shoots and roots were successfully acclimatized in a greenhouse when they were planted in soil.