• 한국식품영양학회지
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• 제12권3호
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• pp.271-278
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• 1999

We isolated activnmycetes LAM-98-80 as strain producing an effective antibiotic for cephalosporin re-sistant pathogenic PSeudomonas sp. and identified as Streptomyces sp. LAM-98-80 from cultural and phyisological characteristics. We investigated the optimal culture conditions for producation of an anti-biotic becoming effective for cephalsporin-resistant pathogenic Pseudomonas sp. It was found that 1.5% soluble starch and 1.0% yeast extract were good as carbon and nitrogen source respectively. The pro-duction of antibiotic was also activated by 0.04% Mn2+ as 80% degree. The optimum initial pH on pro-ductio of antibiotic was pH 7.0. The culture condition for the maximal productivity of the antibiotic was at 3$0^{\circ}C$ for 5 days. The cephalosporin-resistant pathogenic Pseudomonas sp. as test bacteria was rev-ealed to resist antibiotic of cepha families but revealed to not resist those of $\beta$-lactam families ampicil-lin and amoxicillin. Parital purified antibiotic was stable for the pH from 3 to 9 and was also stable when treated at 70 $^{\circ}C$ for 1 hour, This antbiotic was effective against all gram positive and negative bac-teria but was not effective against molds and yeasts.

• Archives of Pharmacal Research
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• 제22권4호
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• pp.391-397
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• 1999

The quaternary ammonium cephalosporin derivatives were prepared with various pyridines substituted at the 3 or/and 4 position. Their in vitro antibacterial activities were determined and substituent effect on pyridine nucleus was studied. Preparation of substituted pyridines are also described.

• 약학회지
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• 제44권4호
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• pp.315-317
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• 2000

The in vitro activities of DA-074, a new cephalosporin against 34 various standard strains and its in vivo efficacies against 6 important strains were obtained. DA-074 showed two fold enhanced in vitro antibacterial activity against some Pseudomonas aeruginosa compared to Ceftazidime and more than 2 fold in vivo efficacy against Staphylococcus aureus Smith, Klebsiella pneumoniae 1 and Escherichia coli KC-14, compared to Cefpirome. DA-074 might be a good candidate for further evaluations.

• 약학회지
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• 제44권4호
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• pp.318-324
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• 2000

9 New cephalosporin derivatives were synthesized and screened for antibacterial activities against various bacteria. (6R,7R) -7$\beta$-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(fluoromethoxyimino)acetamido]-3-[(2-hydroxycarbamoyl)-s-triazolo[1,5-a]-pyrimidin-7-yl]thiomethyl]-3-cephem-4-carboxylic acid sodium salt (compound 3) showed 2 fold enhanced in vitro activity against P. aerurginosa, compared to ceftazidime.

• Bulletin of the Korean Chemical Society
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• 제12권6호
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• pp.674-678
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• 1991

Methanolysis of a ${\beta}$-lactam ring of a cephalosporin was simulated with AM1 semiempirical quantum mechanical calculation. The tetrahedral intermediate TD1 from an O-protonated cephalosporin and a methanol transfers the proton intramolecularly to the C-4 carboxylate to generate an oxyanion, i.e., second tetrahedral intermediate TD2, which undergoes the amide bond cleavage without further protonation on the N-5. For this cleavage a low-energy barrier TS2 was located. According to the energy diagram, tetrahedral intermediates easily undergo ring cleavage even without the protonation on the amide nitrogen.

• 대한화학회지
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• 제38권8호
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• pp.603-607
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• 1994

새로운 cephalosporin 항생물질인 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-[(substituted pyrimidin-2-yl)thiomethyl]-3-cephem-4-carboxylic acid derivatives(2a∼2d)유도체들을 합성하였다. 7-ACA의 3-위치에는 pyridinylthiomethyl기를 도입시키고, 7-위치에는 thiazine를 치환시켜서 구조 변화에 대한 항균 활성을 측정하였다. 그 결과 이들 유도체들은 기준물질인 cefotaxim보다 낮은 항균력을 나타내었다.

• Journal of Microbiology and Biotechnology
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• 제7권2호
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• pp.95-100
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• 1997

• 한국미생물·생명공학회지
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• 제32권3호
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• pp.224-229
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• 2004

토양으로부터 강력한 CAH activity를 갖는 균주를 분리하여, 생화학적, 배양학적, 전자현미경 동정을 한 결과, Bacillus sphaericus로 확인되었으며, 이를 B. sphaericus 366M-9로 명명하였다. 또한 이 균으로부터 최초로 cephalosporin-C deacetylase(CAH)를 분리 정제하였다. 정제수율은 약 7.5% 였으며, B. sphaericus 366M-9에서 분리한 CAH-9의 최적활성 온도는 $50^{\circ}C$였으며, 효소안정 온도구간은 30～$50^{\circ}C$이다. 또한 최적 활성 pH는 7.0이었으며, 효소안정 pH구간은 pH 6.0～8.0으로 90% 이상의 잔존 활성도를 나타내었다. 효소반응속도에 미치는 기질의 영향에서는 $K_{m}$ 값은 0.87 mM 이며,$ V_{max}$는1.22 unit/ml이었다.다.

• 한국미생물·생명공학회지
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• 제17권6호
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• pp.611-618
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• 1989

Cephalosporium acremonium 균주로 미생물 고정화 증식입자를 제조하여 유동층 생물반응기에서 세파로스포린 C 생산에 대한 메치오닌의 영향에 대하여 연구하였다. 메치오닌은 세파로스포린 C 생합성에 매우 중요한 대사조절인자로 알려져 있는데, 본고에서는 초기 발효배지 내 메치오닌 농도의 영향과 이를 토대로 생물반응기에 메치오닌을 주입하였을 때 세파로스포린 C 생산에 미치는 메치오닌의 영향을 관찰하였다. 초기 배지 내에 존재하는 메치오닌에 의해 세파로스포린 C 생산성이 증가하였으며, 메치오닌의 최적양(0.3-0.5w/v％)이 존재하였다. 또한 메치오닌에 의해 탄소원의 소모속도가 증가됨이 관찰되었다. 배지내 메치오닌이 고갈될 때 세파로스포린 C 생산이 극대화되었으나 유동층 생물반응기에서 메치오닌을 부가적으로 첨가하였을 때 그 효과는 기대한 수준에 미치지 못했는데 이는 생체내 메치오닌의 축적과 관계가 있는 것으로 판단되었다. 또 고정화 증식입자를 사용하였을 때 세파로스포린 C 생산에 양호한 결과를 얻었는데 이 경우에도 적정량의 메치오닌 투여가 생산성에 중요한 인자임을 발견하였다. 따라서 유동층 반응기의 운전에 의해 세포로스포린 C 생산성을 향상시키기 위해서는 초기 운전단계에서 최적양의 메치오닌을 주입하는 것이 가장 중요하며 고정화 증식입자의 사용에 의해 공정생산성을 획기적으로 증대시킬 수 있다고 판단되었다.

• 대한미생물학회지
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• 제21권3호
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• pp.375-380
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• 1986

Thirty-one strains of Pseudomonas aeruginosa were submitted to the synergistic activity test of amikacin(AK) and gentamicin(GM) combined with moxalactam(MX), ceftizoxime(CTZ) or cefoperazone(CFZ). The minimal inhibitory concentrations(MICs) of each drug and drugs combined in various ratios were measured by checkerboard dilution method. The synergism was determined through analysing the MIC distribution curve on isobologram and calculating the fractional inhibitory concentration index(FICI). MICs of GM, AK, MX, CFZ and CTZ against the 31 tested strains were distributed from $12.5{\mu}g/ml$ to $800{\mu}g/ml$, from $0.8{\mu}g/ml$ to $25{\mu}g/ml$, from $3.1{\mu}g/ml$ to $50{\mu}g/ml$, from $3.1{\mu}g/ml$ to $400{\mu}g/ml$, and from $12.5{\mu}g/ml$ to $100{\mu}g/ml$, respectively. The rate synergism of each drug combination by means of FICl was 45.5% in GM-MX, 36.4% in GM-CFZ, 63.6% in GM-CTZ, 48.6% in AK-MX, 35.3% in AK-CFZ, and 35.7% in AK-CTZ combination. Thus, it is suggested that Pseudomonas aeruginosa may effectively be inhibited by various aminoglycoside and cephalosporin combinations.