• 대한화학회지
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• 제35권5호
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• pp.575-579
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• 1991

6${\beta}$-bromopenicillanic acid(4a)와 p-nitrobenzylbromide, 3-bromophthalide, chloromethylpivalate 및 1-chlorodiethylcarbonate의 반응으로 6${\beta}$-bromopenicillanates(4b~4e)을 합성하였으며, 6${\beta}$-bromopenicillanic acid(4a)와 그의 ester(4b~4e)를 thioglycolic acid와 친핵성 치환반응시켜 새로운 $\beta$-lactam계 화합물인 6-(carboxymethylthio)penicillanic acid(5a)와 그의 ester(5b~5e)를 얻었다.

• 약학회지
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• 제37권2호
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• pp.158-162
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• 1993

6$\beta$-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl)acetamidopenicillanic acid(7a~7c) and 7$\beta$-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl) acetamidocephalosporanic acid(8a~8c) were synthesized and tested in vitro antibacterial activity. Of these new penicillins exhibited good antibacterial activity against Gram-positive bacteria whereas none of the compounds possessed the activity against Gram-negative bacteria at the concentration tested.

• 한국미생물·생명공학회지
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• 제19권5호
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• pp.439-443
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• 1991

A strain of Streptomyces sp. isolated from soil was found to produce extra-cellular $\beta$-lactamase associated partially to the cell growth. The $\beta$-lactamase was purified from the culture supernatant through anmonium sulfate fractionation, ion-exchange chromatographies and gel filtration. The final purification fold and recovery yield were 57 and 6.2%, respectively. Molecular weight of the $\beta$-lactamase was estimated to be about 67, 000 by SDS-polyacrylamide gel electrophoresis. The optimal reaction condition was at pH 7-8 and at 35-$45^{\circ}C$. The $K_m$ and $V_{max}$ values of the enzyme for penicillin G were estimated to he 3 mM and $3\times 10^3$ $\mu\textrm{M}$/min/mg protein, respectively. The purified $\beta$-lactamase was classified to the class A enzyme hydrolyzing only penicillin.

• 약학회지
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• 제51권6호
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• pp.447-454
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• 2007

The resistance of bacteria against ${\beta}$-lactam antibiotics is mainly caused by the production of ${\beta}$-lactamase enzymes. ${\beta}$-Lactamase inhibitors are used in combination with known antibiotics to overcome the growing problem of bacterial resistance. We prepared 6-(thienylmethylene)penam sulfones for the development of potent ${\beta}$-lactamase inhibitors and evaluated their ${\beta}$-lactamase inhibitory activities.

• 약학회지
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• 제30권5호
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• pp.232-237
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• 1986

A series of modified poly(acrylic acid)'s containing different levels of 6-aminopenicillanic acid (6-APA), 7-aminocephalosporanic acid (7-ACA) and 6-[D-(-)-$\alpha$-aminophenyl acetamido] penicillanic acid (ampicillin) as pendant groups were prepared. Antibiotic activities of the newly prepared drugs were examined against the various gram-positive and gram-negative bacteria. It was found that ampicillin modified composition posses antibiotic activities against the gram-negative as well as the gram-positive bacteria.

• Archives of Pharmacal Research
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• 제14권3호
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• pp.279-281
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• 1991

In the field of cephalosporins, introduction of quaternary heterocyclic methyl goups at the C-3 position has led to a new class of cephalosporins such as cefepime and cefpirome, the so-called 4th generation cephalosporins which are characterized by their potent activity. Since than many efforts were attempted to synthesize more effective analogs.

• 약학회지
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• 제30권1호
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• pp.24-30
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• 1986

New antibiotics having moieties of penicillanic acid, cephalosporanic acid and ampicillin on both ends of the central alkylene were synthesized by reacting 6-aminopenicillanic acid (6-APA), 7-aminocephalosporanic acid (7-ACA) and ampicillin with hexamethylene diisocyanate and sebacoyl chloride, respectively. Antibacterial activities of the compounds were also investigated. The compound derived from sabacic acid and ampicillin exhibited an enhanced antibacterial activities against gram-negative bacteria and was found to be a promising wide-spectrum antibiotic.

• Bulletin of the Korean Chemical Society
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• 제28권7호
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• pp.1085-1086
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• 2007

• Bulletin of the Korean Chemical Society
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• 제30권12호
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• pp.2863-2864
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• 2009

• 대한수의학회지
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• 제25권1호
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• pp.61-67
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• 1985

One hundred and twenty seven strains of Gram-negative rods (72 E. coli, 45 Klebsieila pneumoniae, 8 Enterobacter spp. and 2 Pseudomonas aeruginosa) isolated from bovine mastitis were examined for resistance to ampicilin, carbenicillin and cefazolin, ${\beta}$-lactamase activity and transferable ${\beta}$-lactamase plasmids. Stains resistant to ampicillin were 13.9% in E. coli, 93.3% in Klebsiella pneumoniae, 87.5% in Enterobacter. spp. and all in Pseudomonas aeruginosa, Resistance of E. coli, Klebsiella pneumoniae and Enterobacter spp. to ampicillin was due to the ${\beta}$-lactamases, but all Pseudomonas aeruginosa exhibited a high level of the non-enzymic resistance. Transferable plasmid-mediated ${\beta}$-lactamase synthesis was demonstrated in 61.9% of Klebsiella pneumoniae, 50% of E. coli and 42.9% of Enterobacter spp. The same ${\beta}$-lactamase plasmids specified different resistance levels to various ${\beta}$-lactam antibiotics in different recipients.