• Title/Summary/Keyword: ${\beta}-lactam$

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

  • Young-Min Bae
    • Journal of the Korean Applied Science and Technology
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    • v.39 no.6
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    • pp.916-923
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    • 2022
  • Water samples were collected from three spots(Namcheon, Changwoncheon and Cheongwoonji) in Changwon and genomic DNA was isolated from them. Quantitative PCR was performed with the isolated DNA as template and primers targeting five different class A extended-spectrum beta-lactamase(ESBL) genes(blaOXA-1, blaSHV, blaTEM, blaCTX-M-1, blaCTX-M-9). The number of total ESBL genes from each sample showed large variations between each sample. Thirty nanograms of DNA from Namcheon contained 1.93×106 copies of ESBL genes whereas the same amount of DNA from Changwoncheon contained 1.47×105 copies of ESBL genes. However, the same amount of DNA from Cheongwoonji pond contained only 9.5×103 copies of ESBL genes. The ratio of each ESBL genes showed little difference between Namcheon river and Changwoncheon river, but DNA from Cheongwoonji pond showed a large difference from the rest. blaOXA-1 gene was present at 65.3%, and blaCTX-M-1 gene 33.6% for Namcheon comprising together almost 99%. blaOXA-1 gene was present at 64.1%, and blaCTX-M-1 gene 19.1% for Changwoncheon comprising together over 83%. blaCTX-M-1 gene was present at 87.5% and blaCTX-M-9 genes 9.8% for Cheongwoonji, a pond which is a closed and isolated environment.

The Molecular Mechanical Model of DD-Peptidase

  • Lim, Eongjin;Won, Youngdo
    • Proceedings of the Korean Biophysical Society Conference
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    • 1996.07a
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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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    • v.12 no.6
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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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    • v.8 no.3
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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
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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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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    • 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.

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

  • Chang, Chul Hun;Son, Han Chul;Hwang, Kyu Yon;Park, Kwang Ok;Yang, Ung Suk
    • Quality Improvement in Health Care
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    • v.3 no.2
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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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