• 제목/요약/키워드: Beta-lactam

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Cefadroxil을 사용한 Alkylene Bisdithioureido $\beta$-Lactam 유도체의 합성 및 항균작용 (The Synthesis and Antispectrum of Alkylene Bisthioureido $\beta$-tactam Derivatives of Cefadroxil.)

  • 이기홍;김돈기;김지한;성동호;유주현
    • 한국미생물·생명공학회지
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    • 제17권3호
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    • pp.193-197
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    • 1989
  • Spanner chain의 탄소수가 2,4 또는 6개의 alkylene diisothiocyanate를 합성 후 cefadroxil-2DMF와 반응시켜 spanner chain의 탄소수 2, 4 또는 6개로 연결되어 있고 양쪽에 thioureido group과 $\beta$-lactam ring을 가진 bivalent ligand 구조의 alkylene bisdithioureido $\beta$-lactam 유도체를 합성하고 그 화합물들의 항균작용에 대하여 연구하였다. 그 유도체의 I식 화합물은 $C_{36}$H$_{38}$N$_{8}$O$_{10}$S$_4$, II식 화합물은 $C_{38}$H$_{42}$N$_{8}$O$_{10}$S$_4$, III식 화합물은 $C_{40}$H$_{46}$N$_{8}$O$_{10}$S$_4$의 분자식이다. $\beta$-lactam 감수성 균주에 대한 항균력은 spnner chain의 탄소수가 많을수록 감소하였다.

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새로운 $\beta$-lactam계 항생물질 개발을 위한 검정용 균주의 개발 (Selection of Clinically Isolated Strains for Evaluation of the Newly Synthesized Antibiotics)

  • 김대진;최금화;김숙경;최성숙;김병각;강창율;최응칠
    • 약학회지
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    • 제39권2호
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    • pp.131-136
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    • 1995
  • Clinically isolated bacterial strains resistant to almost of all the clinically superior .betha.-lactam antibiotics can be used to screen the promising ones among the newly synthesized $\beta$-lactam antibiotics. To select the resistant strains, the susceptibility of 389 strains of S. aureus, 144 strains of coagulase negative staphylococci, 509 strains of E. coli, 115 strains of E. cloacae and 187 strains of P. aeruginosa to methicillin, ampicillin, piperacillin and gentamicin was determined. The susceptibility of 19 bacterial strains selected through the first screening to cefixime, cefotiam, cefotaxime, flomoxef, cepfirome, cefdnir, SCE-2787, panipenem and imipenem was determined. Four strains of S. aureus finally selected have high degree of resistance to almost of all $\beta$-lactam antibiotics used and also produce $\beta$-lactamases. These 4 strains of S. aurues can be used to screen effectively the promising $\beta$-lactam antibiotics among the numerous numbers of the newly synthesized $\beta$-lactam antibiotics.

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Staphylococcus aureus에 의한 유방염에 대한 β-lactamase 저해제/β-lactam계 항균제 치료 효과 (Antimicrobial effects of β-lactamase inhibitor/β-lactam antibiotics on staphylococcal mastitis)

  • 임숙경;임재향;주이석;문진산;이애리;고홍범
    • 대한수의학회지
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    • 제43권1호
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    • pp.113-120
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    • 2003
  • The antimicrobial effect of ${\beta}$-lactam antibiotics, which had ${\beta}$-lactamase inhibitor activity, on Staphylococcus aureus isolated from mastitis was investigated in this study. Out of 166 isolates, 99 isolates (59.6%) produced ${\beta}$-lactamase, and 98 isolates of 99 were ${\beta}$-lactamase positive in above $12.5{\mu}g/m{\ell}$ MIC of penicillin. In the providence distribution, ${\beta}$-lactamase production rate of 4 providence, Gangwon, Gyeonggi, Chungcheong, and Jeolla was 100%, 65.7%, 58.8%, and 50.0%, respectively. Antibiotic activities of ${\beta}$-lactam antibiotics against lactamase positive isolates also were investigated. Antimicrobial effects of ampicillin/sulbactam or amoxicillin/clavulanic acid treated group were better than ampicillin or amoxicillin treated group. In antimicrobial effects on intracellular S aureus, there was no difference 1 hour and 4 hour treatment in control, ampicillin, and amoxicillin group, but in 18 hours treatment, ampicillin/sulbactam or amoxicillin/clavulanic acid had a better effect than ampicillin or amoxicillin (p<0.05).

Detection of $\beta$-lactam Antibiotic-resistant Genes in Eschericia coli using DNA Chip from Porcine Fecal Samples

  • Na, Sung-ho;Cho, Ho-seong;Kim, Yong-hwan;A.W.E. Effendy;Park, Nam-yong
    • 한국수의병리학회:학술대회논문집
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    • 한국수의병리학회 2003년도 추계학술대회초록집
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    • pp.33-33
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    • 2003
  • There prevalence of $\beta$-lactamases bacteria in animals has been increased since 1990s [1]. The resistance in E coli which is mediated by $\beta$-lactamases hydrolyze the $\beta$-lactam ring eventually inactivate the antibiotics [2]. Generally, $\beta$-lactamases can be classified into four main groups and eight subgroups according to their functional and structural characteristics [3]. The detection of $\beta$-lactam antibiotic-resistant bacteria by DNA chip has been described [4]. The chip has a specific probe DNAs that contained the $\beta$-lactam antibiotic-resistant genes which was labeled by multiplex PCR reaction with a mixture of primer sets that were designed to amplify specific gene. Here we report the susceptibility of enteropathogenic E. coli isolated from pigs in Korea using the DNA chip in detecting $\beta$-lactam antibiotic-resistant genes. (omitted)

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A novel method to depurate β-lactam antibiotic residues by administration of a broad-spectrum β-lactamase enzyme in fish tissues

  • Choe, Young-Sik;Lee, Ji-Hoon;Jo, Soo-Geun;Park, Kwan Ha
    • Fisheries and Aquatic Sciences
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    • 제19권10호
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    • pp.45.1-45.5
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    • 2016
  • As a novel strategy to remove ${\beta}$-lactam antibiotic residues from fish tissues, utilization of ${\beta}$-lactamase, enzyme that normally degrades ${\beta}$-lactam structure-containing drugs, was explored. The enzyme (TEM-52) selectively degraded ${\beta}$-lactam antibiotics but was completely inactive against tetracycline-, quinolone-, macrolide-, or aminoglycoside-structured antibacterials. After simultaneous administration of the enzyme with cefazolin (a ${\beta}$-lactam antibiotic) to the carp, significantly lowered tissue cefazolin levels were observed. It was confirmed that the enzyme successfully reached the general circulation after intraperitoneal administration, as the carp serum obtained after enzyme injection could also degrade cefazolin ex vivo. These results suggest that antibiotics-degrading enzymes can be good candidates for antibiotic residue depuration.

방선균의 일주가 생성하는 $\beta$-Lactamase Inhibitor의 특성 (Characters of $\beta$-Lactamase Inhibitor Produced by Streptomyces sp.)

  • 김종찬;곽무영;이정상;이호설
    • 한국미생물·생명공학회지
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    • 제16권5호
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    • pp.398-401
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    • 1988
  • $\beta$-lactamase을 저해하는 물질을 생성하는 방선균의 일균주를 토양에서 분리하였다. 분리된 균으로부터 $\beta$-lactamase 저해물질을 생산하는 조건을 검토하였고, 아울러 배양액에서부터 동 물질을 분리정제하여 그 특성의 일부를 조사하였다. 그 결과 이 물질은 $\beta$-lactam ring을 가지고 있지 않았으며, $\beta$-lactam 항생물질에 대한 내성을 나타내는 E. coli 내성균주에 강한 항생력을 나타냄을 알았다.

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부산지역 하천에서 분리된 장내세균 Escherichia coli와 Klebsiella pneumoniae의 광범위 베타 락탐 분해효소 (Extended-Spectrum ${\beta}-Lactamase$)에 대한 유형별 분류 (Typing of Extended-Spectrum ${\beta}-Lactamase$ of Escherichia coli and Klebsiella pneumoniae Isolated from Rivers in Busan, Korea)

  • 이훈구;김혜진;김군도
    • 미생물학회지
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    • 제43권2호
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    • pp.116-123
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    • 2007
  • 본 연구는 부산지역 하천에서 plasmid 매개성 광범위 ${\beta}-lactam$ 분해효소(extended spectrum ${\beta}-lactamase;\;ESBL$)를 생성하는 세균을 분리하여 생성된 광범위 ${\beta}-lactam$ 분해효소를 유형별로 분류하기 위함이다. Escherichia coli 6균주와 Klebsiella pneumoniae 15균주가 피전달균주인 Escherichia coli J53 $Azid^{R}$에 plasmid 매개성 광범위 ${\beta}-lactam$ 분해효소 생성 인자를 전달하였다. PCR 후 얻은 유전인자를 plasmid로 매개된 광범위 ${\beta}-lactam$ 분해효소 유전자의 염기서열 분석결과, E. coli와 K. pneumoniae 유전자를 BCM Search Launcher 및 GenBank nucleotide database를 통하여 검색한 결과 ESBL 유형은 TEM-52형과 SHV-12형이었다. TEM-52는 E. coli와 K. pneumoniae 양쪽에서 분리되었다. 그러나 SHV-12는 K. pneumoniae에서만 분리되었다. 이상의 결과로부터 plasmid 매개성 광범위 ${\beta}-lactam$ 분해효소를 생성하는 세균이 한국에서는 이미 임상범위를 넘어 자연계까지 확산되었음을 알 수 있었다.

GC/FPD를 이용한 $\beta$-락탐계 항생물질의 분석(I) (Determination of $\beta$-Lactam Antibiotics by Gas Chromatography with Flame Photometric Detector (I))

  • 박만기;조영현;양정선
    • 약학회지
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    • 제28권1호
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    • pp.25-27
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    • 1984
  • Some $\betha$-lactam antibiotics-penicillins and cephalosporins-were determined by gas chromatography (GC) with flame photometric detector (FPD) which was selective and sensitive to sulfur-containing compounds. Methyl ester derivatives of carboxyl group in $\betha$-lactam antibiotics were prepared using 0.5Mmethyl iodide in methylene chloride and were taken for gas chromatography with 0.9% or 0.6% QF-1 on Chromosorb WAW-DMCS. We have found that it is possible to determine methyl esters of $\betha$-lactam antibiotics by GC/FPD.

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Computer Graphics / Molecular Mechanics Studies of ${\beta}$-Lactam Antibiotics. Geometry Comparison with X-Ray Crystal Structures

  • Chung, Sung-Kee;Chodosh, Daniel F.
    • Bulletin of the Korean Chemical Society
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    • 제10권2호
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    • pp.185-190
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    • 1989
  • Geometries for a number of representative ${\beta}$ -lactam antibiotics (penams, cephems and monobactams) have been calculated by computer graphics/molecular mechanics energy minimization procedures using both MM2 and AMBER force fields. The calculated geometries have been found in reasonable agreement with the geometries reported in the X-ray crystal structures, especially in terms of the pyramidal character of the amide nitrogen in the ${\beta}$-lactam ring and the Cohen distance. Based on these calculations, it is suggested that the nitrogen atom in the monobactams may also have pyramidal geometries in the biologically active conformations.

Detection of beta-lactam antibiotic resistant genes in Escherichia coli from porcine fecal samples using DNA chip

  • Park, Nam-Yong;Na, Sung-Ho;Cho, Ho-Seong
    • 한국동물위생학회지
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    • 제30권4호
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    • pp.505-510
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    • 2007
  • This study was conducted to detect ${\beta}$-lactam antibiotic-resistant genes in the 400 E coli isolates from porcine fecal samples in Korea by a DNA chip. The DNA chip contains the specific probe DNAs of the ${\beta}$-lactam antibiotic-resistant genes that had been labeled with a mixture of primer set designed to amplify specific genes (PSE, OXA, FOX, MEN, CMY, TEM, SHV, OXY and AmpC) using a multiplex polymerase chain reaction (PCR). Of 400 isolates 339 contained at least one ${\beta}$-lactamases gene. Resistance to ${\beta}$-lactamases was mediated mainly by AmpC (n = 339, 100%), and followed by TEM (n = 200, 59.0%), CMY (n = 101, 29.8%), PSE (n = 30, 8.9%) and both OXA and SHV genes (n = 20, 5.9%), while the FOX, MEN and OXY genes were not detected. The other sixty-one did not contain any ${\beta}$-lactamase genes even though they were resistant to antimicrobial drugs. In conclusion, the DNA chip system can be used as a rapid and reliable method for detecting of ${\beta}$-lactamases genes, which will help veterinarians select the antibiotics for monitoring and treating of animal diseases.