• 제목/요약/키워드: ${\beta}$-lactam

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주변 수계에서 미생물유래 extended-spectrum beta-lactamase 유전자의 분포 (Distribution of the extended-spectrum beta-lactamase genes derived from microorganisms in the waterfront environments)

  • 배영민
    • 한국응용과학기술학회지
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    • 제39권6호
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    • pp.916-923
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    • 2022
  • 창원시의 3개 지점(남천, 창원천, 청운지)에서 물 시료를 채취하고, 채취한 시료로부터 genomic DNA를 분리하였다. 분리된 DNA와 class A extended-spectrum beta-lactamase(ESBL) 유전자 5가지(blaOXA-1, blaSHV, blaTEM, blaCTX-M-1, blaCTX-M-9)를 target으로 하는 primers를 사용하여 quantitative PCR을 수행하였다. 시료를 채취한 지점별로 ESBL 유전자들의 수와 비율에서 확연한 차이가 있음을 알 수 있었다. 남천의 경우 DNA 30ng당 ESBL 유전자가 1.93×106 copy나 존재하는 데에 반해 창원천의 경우에는 1.47×105 copy 그리고 청운지에는 9.5×103 copy 밖에 존재하지 않았다. 흐르는 하천인 남천과 창원천에서는 각 ESBL 유전자들의 비율에서 큰 차이가 없었다. 즉, 남천에서는 blaOXA-1 유전자가 65.3%, blaCTX-M-1 유전자가 33.6%를 차지하여서 이 두 유전자가 전체 ESBL 유전자의 99% 가까이를 차지하고 있었다. 창원천에서도 blaOXA-1 유전자가 64.1%, blaCTX-M-1 유전자가 19.1%를 차지하므로 이 두 유전자가 전체의 83% 이상을 차지하고 있었다. 하천과 다르게 폐쇄된 환경인 청운지 연못에서는 내성세균들의 총량 자체가 다른 두 하천에 비해서 월등하게 적었다. 또한 내성 세균의 비율도 달라서 blaCTX-M-1 유전자가 전체의 87.5%, 그리고 blaCTX-M-9 유전자가 9.8%를 차지하고 있었다.

The Molecular Mechanical Model of DD-Peptidase

  • Lim, Eongjin;Won, Youngdo
    • 한국생물물리학회:학술대회논문집
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    • 한국생물물리학회 1996년도 정기총회 및 학술발표회
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    • pp.22-22
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    • 1996
  • In order to establish the structural requirements for designing new ${\beta}$-lactam antibiotics it is necessary to build the molecular model of a penicillin binding protein. D-alanyl-D-alanine carboxypeptidase/transpeptidase (DD-peptidase) is a good model for PBPs. The X -ray crystallographic structure of DD-peptidase has been reported at the 1.6${\AA}$ resolution. (omitted)

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Theoretical Studies on the Methanolysis of a Cephalosporin; Mimicking Acylation of the Active Site Serine of D-Ala-D-Ala Transpeptidases

  • Nahm, Kee-Pyung
    • 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.

Synthetic beta-Lactam Antibiotics I. Synthesis and Antibacterial Activity of 7-Amino-3-[1-(halo-substituted phenyl)-1H-tetrazole-5-yl]thiomethyl-3-cepheme-4-carboxylic acids

  • Koh, Dong-Soo;Park, Sang-Woo;Kim, You-Seung
    • Bulletin of the Korean Chemical Society
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    • 제8권3호
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    • pp.189-192
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    • 1987
  • The syntheses of mercaptotetrazoles and cephalothin analogs are described. Their in vitro potency was established. The compounds exhibited high antibacterial activity against Gram-positive bacteria and moderate activity against Gram-negative bacteria.

SYNTHETIC DEVELOPMENT OF NEW 1$\beta$-SUBSTITUTED CARBAPENEMS

  • Nagao, Yoshimitsu
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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    • pp.34-35
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    • 1993
  • The Development of new asymmetric induction methods useful for syntheses of biologically active natural products and drugs, using C4-chiral 1,3-th-iazolidine-2-thiones, has been a recent focus of interest. 1-8) The present account describes the significance of particular heterocycles in the synthetic development of new 1${\beta}$-substituted carbapenems. A fungal metabolite, (+)-thienamycin (1) has attracted one's attention as a hopeful candidate for new-generation antibiotic drugs because of its strong antimicrobial activities and wide antimicrobial spectra due to the extensive inhibition against various ${\beta}$-lactamases. However, it has been serious problems toward a practically useful drug that (+)-thienamycin is fairly labile in the solution and can be metabolized by renal dehydropept- idase-I (DHP-I). Recently, a Merck Sharp & Dohme research group exploited a non-natural ${\beta}$-lactam, imipenem (2) which has been appeared in the drug market as the first carbapenem-type antibiotic drug. 9) However 2 must be used with a DHP-I inhibitor, cilastatin sodium (3).9) Thus, a 1,${\beta}$-methyl- carbapenem derivative 4 has been disclosed by the same group. 10) It seems to be more hopeful candidate as a new-generation antibiotic because it can directly resist against metabolism by the renal DHP-1 without an enzyme inhibitor 3. 10)

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Preparation of biodegradable microspheres containing water-soluble drug, $\beta$-lactam$ antibiotic

  • Kim, Jin-Hee;Kwon, Ick-Chan;La, Sung-Bum;Jeong, Seo-Young;Young, Taek-Sohn;Seo, Young-Jeong
    • Archives of Pharmacal Research
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    • 제19권1호
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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.

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감염증 환자에서 vancomycin, teicoplanin 투여례에 대한 연구 - 항균제 투여의 적응증 평가 - (Study on patients of infectious diseases administered with vancomycin or teicoplanin - Assessment of fitness of antimicrobial administration -)

  • 장철훈;손한철;황규연;박광옥;양웅석
    • 한국의료질향상학회지
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    • 제3권2호
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    • pp.26-35
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    • 1997
  • Background : Glycopeptide antibiotics are the only drugs for treatment of infections due to beta-lactam-resistant Gram-positive bacteria. As the incidence of infection and colonization with vancomycin-resistant enterococci(VRE) rapidly increases, the hospital infection control practices advisory committee(HICPAC) recommends prudent vancomycin use to detect, prevent and control infection and colonization with VRE. Methods : The inpatients admitted from September to December, 1996 in Pusan National University Hospital, with Gram-positive bacterial infections were evaluated retrospectively to see whether the administrations of glycopeptide antibiotics were appropriate or not, upon comparison with the recommendations for preventing the spread of vancomycin resistance by HICPAC. Results : Teicoplanin has been chosen more frequently than vancomycin of the glycopeptide antibiotics. The indications of administration of glycopeptides in patients with pneumonia, wound infections, sepsis, and in febrile or neutropenic patients with malignancies were appropriate, but the use of glycopeptides for elimination of merely colonized bacteria in the oral cavity could not be excluded. Inappropriate use of glycopeptides was 10.6%, and inappropriately long-term use without positive culture for beta-lactam-resistant Gram-positive organisms was about 40% of total days of drug use. Conclusion : It seems essential for the quality assurance committee to make a plan in teaching the HICPAC recommendations to the medical practitioners who prescribed the glycopeptides inappropriately or used for irrelevantly long to his patient, monitor and survey their use of glycopeptides prospectively and periodically, and if there are repeated inappropriate prescriptions, a certain penalty would be given to the practitioners.

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