• 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.11 no.4
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• pp.271-273
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• 1990

• Journal of Microbiology and Biotechnology
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• v.29 no.3
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• pp.465-472
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• 2019

Several reports describe antimicrobial-resistance transfer among children and the community in outbreak situations, but transfer between a child and a caregiver has not been examined in child care facilities under normal circumstances. We investigated the transfer of antimicrobial-resistance genes, resistant bacteria, or both among healthy children and teachers. From 2007 to 2009, 104 Escherichia coli isolates were obtained from four teachers and 38 children in a child care center. Twenty-six cephem-resistant isolates were obtained from children in 2007 and 2008. In 2009, cephem-resistant isolates were detected in children as well as a teacher. Nalidixic acid-resistant isolates from the same teacher for 3 years showed low similarity (<50%) to each other. However, an isolate from a teacher in 2007 and another from a child in 2008 showed high similarity (87%). Pulsed-field gel electrophoresis revealed 100% similarity for four isolates in 2007 and one isolate in 2008, and also similarity among seven isolates carrying the virulence gene (CNF1). This study yielded the following findings: (1) a gene for extended-spectrum ${\beta}$-lactamase was transferred from a child to other children and a teacher; (2) a nalidixic acid-resistant isolate was transferred from a teacher to a child; and (3) a virulent bacterium was transferred between children.

• Archives of Pharmacal Research
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• v.20 no.3
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• pp.288-290
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• 1997

An efficient synthesis of 3-(E)-hydroxy- and 3-(E)-acetoxypropenylcephem derivatives, key intermediates for the synthesis of 3-(E)-propenylcephalosporins was achieved via Stille coupling reaction of 3-trifloxycephem with 3-(E)-tributylstannylallylic alcohol.

• YAKHAK HOEJI
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• v.44 no.4
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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.

• Proceedings of the PSK Conference
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• 2000.10a
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• pp.210.3-211
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• 2000

• Bulletin of the Korean Chemical Society
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• v.11 no.4
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• pp.323-327
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• 1990

The synthesis and some biological properties of $7{\beta} $-[2-(Z)-(2-aminothiazole-4-yl)-2-(N-substitutedcar bonyl)ethoxyiminoacetamido]-3-vinyl-3-cephem-4- carboxylic acid are described. The effect of substituents on the carbamoly group in the 7-side chain were investigated in order to improve antibacterial activities. Two of these new orally active $7{\beta} $-lactam derivatives showed wide expanded antimicrobial activities against Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa, as well as good stability to $7{\beta} $ -lactamases.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.120-120
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• 1993

목적: Aminothiazole-oxime type의 세파로스 포린계 항생제가 개발되어 제3, 4세대 항생제로 쓰이고 있거나 개발중에 있다. 본 저자들은 pseudomonas균에도 항균력이 우수하고 $\beta$-Iactamase에도 안전하며 기존에 보고된 화합물 보다 개선된 약물을 찾으려는 시도에서 본 연구를 실시하였다. 방법: Cephem의 C-7위치에 aminothiazole methoximetype를 도입시키고C-3위치에 약리 활성이 기대되는 5-(aryl or hot.)-4-phony고-3-mercapto-4H-1,2,4-triazole 화합물들을 합성하여 도입시켜 gram(＋), gram(－) 및 fungus균에 대하여 항균력을 실험 하였다. 결과: 합성된 복합물들의 항균력 판정은 Pseudomonas균에는 항균력이 대조 물질 보다 떨어졌으나 몇몇균에 대해서는 대조물질과 비슷한 항균력을 나타내었다.

• Journal of the Korean Applied Science and Technology
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• v.6 no.1
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• pp.27-30
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• 1989

The fast separation and determination of cefatrizine${\cdot}$propylene glycol and inmpurities - TACA: 7-amino-3-(1,2,3-triazol-4-yl)thiomethyl-3-cephem-4-carboxylic acid and 7-ACA; 7-amino cephalosporanic acid - was performed by the high poerformance liquid chromatography using octadecyl siland (ODS) column. Methanol and ammonium phosphate buffer [$0.03M(NH_4)_2\;HPO_4$, (pH 7.5)] was used analyze, as eluent. The experimental value of the contents of cefatrizine${\cdot}$propylene glycol and impurities agree with the theoretical value of those.

• Bulletin of the Korean Chemical Society
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• v.15 no.6
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• pp.453-455
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• 1994

Semiempirical MO calculations are applied to estimate the substituent effects on acylations of the nonfused N-vinyl-2-amino $\beta-lactams$ having frameworks analogous to 3-cephems. The stabilization energy for the reaction intermediate of the nucleophilic attack by the hydroxide ion is selected as the reactivity index and calculated by AM1 and PM3 methods for the model $\beta-lactams$ with substituents at the C1 and N-vinyl terminal positions. The reactivities are larger for -SH connected to the C1 and strong $\pi-acceptors$ at the N-vinyl terminal implying the large reactivity for known active cephalosporins. Quantum chemical calculation of stabilization energy could be useful in correlating antibiotic activities of many compounds obtained as derivatives of a lead compound.