• Archives of Pharmacal Research
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• v.13 no.4
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• pp.385-387
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• 1990

3-[(1-Methyl-1H-tetrazol-5-y)thiomethyl] is one of the most important side chains in cephaloporins. This side chain which occures in numerous antibacterial agents, suc as cefamandole, latamoxef, cefoperazone, and cefmenoxime, contributes remarkable potency and broad spectrum. For the continuous work of study on the development of broad spectrum cephalosporins, we become interested in the effect of structural modification of the substituent at the N-1 position of mercaptoterazole toward biological activity because our recent work had demonstraated that the arylsubstituted mercaptotetrazoles (Fig. 1) had favorable effect on the activity against gram-positive bacteria. The main focus of this report was to investigate the relationship between activity and functional groups in the mercaptotetrazole.

• 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.15 no.2
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• pp.187-189
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• 1992

In the preceding paper, we reported the synthessis and biological properties of cephalosporins having quinoliniumthiomethyls at the C-3 position and demonstrated that quinoliniumthiomethylcephalosporins exhibited an extended antibacterial spectrum including antipseudomonal activity, especially strong antiGram-positive activity. With the aim of elaboration to optimize the antibacterial potency of the quaternary ammonium cephalosporins, we have studied the modification of substituents in the pyrrolidine ring of cefepime 1 which is characterized by its potent activity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.26 no.6
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• pp.886-893
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• 2012

Methicillin-Resistant Staphylococcus aureus (MRSA) is a cephalosporin and beta-lactam antibiotic-resistant strain. In most cases, MRSA is spread from infected patients and infection rates are growing increasingly. Furthermore, increased resistance to antibiotics is causing serious problems in the world. Staphylococcus aureus is responsible for both nosocomial and community-based infections that range from relatively minor skin and soft tissue infections to life-threatening systemic infections. Therefore, there is a need to develop alternative antimicrobial drugs for the treatment of infectious diseases. In this study, we investigated antimicrobial activity of oriental medicine prescription against MRSA. The minimum inhibitory concentration (MIC) of Sohamhyung-tang water extract against S. aureus strains ranged from 500 to 2,000 ${\mu}g/mL$, so we have it confirmed that a strong antibacterial effect. Also, the combinations of Sohamhyung-tang water extract and conventional antibiotics exhibited improved inhibition of MRSA with synergy effect. We suggest that Sohamhyung-tang water extract against MRSA have antibacterial activity, it has potential as alternatives to antibiotic agent. We suggest that the Sohamhyung-tang water extract lead the treatment of bacterial infection to solve the resistance and remaining side-effect problems that are the major weak points of traditional antibiotics.

• Journal of Life Science
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• v.22 no.9
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• pp.1268-1276
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• 2012

The emergence and dissemination of carbapenem-resistant bacteria have resulted in limitations of antibiotic treatment and potential outbreaks of metallo-${\beta}$-lactamase (MBL) producing Pseudomonas aeruginosa resistant to carbapenems. In this study, we conducted molecular characterization of the MBL genes of the ${\beta}$-lactam drug-resistant P. aeruginosa and prepared basic data for treatment and prevention of proliferation of antimicrobial-resistant bacterial infections. Forty-two P. aeruginosa isolates of 254 were resistant to imipenem or meropenem. Among the 42 isolates, 28 isolates were positive for the Hodge test, and 23 isolates were positive for the EDTA-disk synergy test (EDST). MBLs were detected in 59.5% (25/42) of P. aeruginosa isolates. Eight isolates harbored $bla_{IMP-6}$, whereas 17 isolates harbored $bla_{VIM-2}$. The $bla_{IMP-6}$ gene was in a class 1 integron containing five gene cassettes: $bla_{IMP-6}$, qac, aacA4, $bla_{OXA-1}$, and aadA1. Some strains that produce IMP-6 and VIM-2 showed epidemiological relationships. The $bla_{IMP-6}$ gene in carbapenem-resistant P. aeruginosa showed an identical pattern to a gene cassette that was reported at a hospital in Daegu, Korea. Therefore, MBL-producing P. aeruginosa is already endemic in the community. We are concerned that the existence of carbapenem-resistant bacteria containing the blaMBL gene may increase pressure on antibiotic selection when treating infections. We believe that we should select appropriate antibiotics based on the antibiotic susceptibility test and continue the research to prohibit the emergence and spread of antibiotics resistant bacteria.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.30-35
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• 1996

Poly(l-lactic acid)(PLLA) microspheres loaded with ampicillin sodium (AMP-Na_, .betha.-lactam antibiotic, were prepared by a w/o/w multiple emulsion-solvent evaporation method. The amounts of each component in three phases (inner water phase, organic phase, and outer water phase) wre carefully examined in the preparation of PLLA microspheres. The stirring rate, another preparation parameter, was also investigated for study on the effect of mechanical stress on the drug loading and morphology of PLLA microspheres. Most of the preparation parameters had a great influence on the drug loading, surface morphology and size distribution of PLLA microspheres. PLLA microspheres with 15.89 w/w% drug loading were subjected to the in vitro release experimet. The release of ampicillin sodium was constant at a rate of 1.68 $mug/ml/day$ per 1 mg of microspheres for 18 days initial burst effect.

• YAKHAK HOEJI
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• v.49 no.1
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• pp.51-55
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• 2005

In vitro ${\beta}$-lactamase inhibitory activity of 6-triazole exomethylenepenam compounds (1, 2, 3, 4, 5 and 6) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of 3, 4 and 5 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type IV enzymes. And, inhibitory activity of 3 and 4 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type III enzymes. The in vitro antimicrobial activity of 3, 4 and 5 combined with ampicillin was better than those with sulbactam and with cefoperazone was compared with the sulbactam against ${\beta}$-lactamase producing 27 strains. The synergistic activity of (Z)-form compounds (3 and 5) was better than that of (E)-form compound (4) and sulfone compound (5) was better than sulfide compound (3).

• Journal of Life Science
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• v.27 no.10
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• pp.1145-1151
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• 2017

In this study, we report on a simple, efficient method for obtaining penicillin G amidase (PGA) from recombinant Escherichia coli using a formulation mixed with detergent and lysozyme. Research was conducted on the extraction efficiency of PGA from the periplasmic space in cells in terms of the type of detergent, detergent concentration, pH, reaction time, and temperature of permeabilization. The extraction yield of PGA in the formulated surfactant/lysozyme treatment was increased by approximately (55-65 U/ml) in comparison with that in the single surfactant treatment. The released PGA solution was concentrated and exchanged with buffer using an ultrafiltration (U/F) system. The yields of diatomite filtration, membrane filtration (M/F), and U/F were 69.7%, 93.8%, and 77.3%, respectively. A total of 212 KU of PGA was recovered. At the 25-L culture scale, the overall yield of extraction using the mixed surfactant/lysozyme method was 49.2%. The specific activity of extracted PGA was 11 U/mg in protein. The concentrated PGA solution was immobilized on microporous silica beads without further purification of PGA. The total immobilization yield of PGA on the resin was 48.7%, while the enzyme activity was 101 U/g. The immobilized PGA was successfully used to produce 6-APA from penicillin G. Our results indicated that a simple extraction method from periplasmic space in E. coli may be used for the commercial scale production of ${\beta}-lactam$ antibiotics using immobilized PGA.

• YAKHAK HOEJI
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• v.40 no.1
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• pp.102-111
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• 1996

LB10522 is a new parenteral broad spectrum cephalosporin with a catechol moiety at C-7 position of beta-lactam ring. This compound can utilize tonB-dependent iron transp ort system in addition to porin proteins to enter bacterial periplasmic space and access to penicillin-binding proteins (PBPs) which are the lethal targets of ${\beta}$-lactam antibiotics. The chelating activity of LB10522 to metal iron was measured by spectrophotometrically scanning the absorbance from 200 to 900nm. When $FeCl_3$ was added, optical density was increased between 450 and 800nm. LB10522 was more active against gram-negative strains in iron-depleted media than in iron-replete media. This is due to the increased expression of iron transport channels in iron-depleted condition. LB10522 showed a similar activity against E. coli DC2 (permeability mutant) and E. coli DCO (wild type strain) in both iron-depleted and iron-replete media, indicating a minimal permeaility barrier for LB10522 uptake. LB10522 had high affinities to PBP 3 and PBP 1A, 1B of E. coli. By blocking these proteins, LB10522 caused inhibition of cell division and the eventual death of cells. This result was correlated well with the morphological changes in E. coli exposed to LB10522. Although the in vitro MIC of LB10522 against P. aeruginosa 1912E mutant (tonB) was 8-times higher than that of the P. aeruginosa 1912E parent strain, LB10522 showed a similar in vivo protection efficacy against both strains in the mouse systemic infection model. This result suggested that tonB mutant, which requires a high level of iron for normal growth, might have a difficulty in surviving in their host with an iron-limited environment.

• Korean Journal of Veterinary Service
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• v.29 no.3
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• pp.331-338
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• 2006

This survey was carried out to detect the residual antibiotics in beef (n = 1,071), pork (n=7,837) and chicken (n=1,536) from slaughter houses in Gyeongbuk province by EEC-4 plate method, Charm II and HPLC during 2005. Residues of antibiotic were detected from 9 beef (0.8%) and 119pork (1.52%) by EEC-4 plate method, and total positive rates were 1.23% (128). 126 samples of the 128 positive samples by the EEC-4 plate method were detected by charm II test. 128 samples were classified as tetracyclines 110 (95.5%), ${\beta}$-lactam 2 (1.6%), sulfonamide 22 (17.2%), quinolone 1 (0.8%). The highest residual concentration of oxytetracycline, tetracycline, chlor-tetracycline, penicillin, sulfamethazine, sulfadimethoxine, sulfaquinoxaline, sulfamerazine, sulfamonomethoxine and enrofloxacin were 7.57, 0.27, 0.40, 0.24, 14.24, 4.33, 8.59, 0.12, 0.09 and 1.98 ppm, respectively and 49 samples were exceeded legal admitted levels.