• 제목/요약/키워드: beta-lactams

검색결과 57건 처리시간 0.026초

서울에서 도축된 소의 잔류항생물질 비교조사 (Comparison of residual antibiotics in slaughtered cattle in Seoul)

  • 김보숙;김기근;이병동
    • 한국동물위생학회지
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    • 제22권2호
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    • pp.105-111
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    • 1999
  • This survey was carried out to detect the residual antibiotics in muscles of slaughter cattle from slaughter houses in Seoul from 1991 to 1998 using by EEC-4-plate method. The results were summarized as follows ; 1. Residual materials were detected in 402 samples(3.12%) by EEC-4-plate method. The detection ratios were highest in 1995 (9.51%), autumn (39.8%), Kyeonggi province (54.2%), Holestain(60.4%) and male(50.7%). 2. Residual antibiotics for 18 samples were classified as TCs(72.2%), sulfonamides(38.8% ) and $\beta$-lactams(5.5%) by HPLC 3. The residual concentration of oxytetracycline, sulfonamide and $\beta$-lactams were 0.34~15.93ppm, 0.17~1.18ppm and 0.06ppm, respectively.

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Semiempirical Molecular Orbital Calculations of the Substituent Effects on Acylations of 3-Cephem Analogues

  • Chang Moon-Ho;Koh Hun-Yeong;Lee Jung-Chull;Lee Yoon Sup
    • Bulletin of the Korean Chemical Society
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    • 제15권6호
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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.

Structural Insights for β-Lactam Antibiotics

  • Dogyeoung, Kim;Sumin, Kim;Yongdae, Kwon;Yeseul, Kim;Hyunjae, Park;Kiwoong, Kwak;Hyeonmin, Lee;Jung Hun, Lee;Kyung-Min, Jang;Donghak, Kim;Sang Hee, Lee;Lin-Woo, Kang
    • Biomolecules & Therapeutics
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    • 제31권2호
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    • pp.141-147
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    • 2023
  • Antibiotic resistance has emerged as a global threat to modern healthcare systems and has nullified many commonly used antibiotics. β-Lactam antibiotics are among the most successful and occupy approximately two-thirds of the prescription antibiotic market. They inhibit the synthesis of the peptidoglycan layer in the bacterial cell wall by mimicking the D-Ala-D-Ala in the pentapeptide crosslinking neighboring glycan chains. To date, various β-lactam antibiotics have been developed to increase the spectrum of activity and evade drug resistance. This review emphasizes the three-dimensional structural characteristics of β-lactam antibiotics regarding the overall scaffold, working mechanism, chemical diversity, and hydrolysis mechanism by β-lactamases. The structural insight into various β-lactams will provide an in-depth understanding of the antibacterial efficacy and susceptibility to drug resistance in multidrug-resistant bacteria and help to develop better β-lactam antibiotics and inhibitors.

Flexible docking of stereoisomers of allyl substituted penam sultones into metallo-$\beta$-lactamase with QXP

  • Choi, In-Hee;Kim, Ji-Hyun;Kim, Choon-Mi
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.314.1-314.1
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    • 2002
  • Bacterial ${\beta}$-lactamases provide resistance to ${\beta}$-lactams by hydrolyzing the ${\beta}$-lactam bond, On the basis of their catalytic mechanisms. ${\beta}$-lactamases are divided into two major groups. Class A. C and D which belong to the first group require serine in the active site and class B which is the second group require Zn(II) for their activity. Among class B enzymes, Bacteroides fragilis ${\beta}$-lactamase (CcrA enzyme) require two Zn(II) ions per monomer for maximal enzymatic activities. (omitted)

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The Synergistic Antibacterial Activity of 1-Acetyl-$\beta$-Carboline and $\beta$-Lactams Against Methicillin-Resistant Staphylococcus aureus (MRSA)

  • Shin, Hee-Jae;Lee, Hyi-Seung;Lee, Dae-Sung
    • Journal of Microbiology and Biotechnology
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    • 제20권3호
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    • pp.501-505
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    • 2010
  • 1-Acetyl-$\beta$-carboline was isolated as an anti-MRSA agent from the fermentation broth of a marine actinomycete isolated from marine sediment. The producing strain was identified to be Streptomyces sp. by phylogenetic analysis of the 16S rRNA gene sequence. The anti-MRSA agent was isolated by bioactivity-guided fractionation of the culture extract by solvent partitioning, ODS open flash chromatography, and purification with a reversed-phase HPLC. Its structure was elucidated by extensive 2D NMR and mass spectral analyses. Combination of 1-acetyl-$\beta$-carboline with ampicillin exhibited synergistic antibacterial activity against MRSA.