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

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Quinolone 계 화합물의 개발

  • 함원훈
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1992.05a
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    • pp.17-17
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    • 1992
  • 항균성 물질을 이용한 화학 요법의 역사는 1930 년대 초 술폰아미드의 발견으로부터 비롯되었고, 페니실린의 발견 이래 $\beta$-lactam 계 항생제가 주종을 이루고 있다. 1963년 Lesher 와 Gruett 에 의해 합성된 nalidixic acid 가 요도염 치료제로 임상에 사용된 이후 이와 유사한 구조를 갖는 항균제 개발에 많은 연구가 진행되어 제 1세대, 제 2세대의 quinolone 개발에 이어 1950년대에 들어 제 3세대 quinolone의 개발이 활발히 진행되어 왔다. 제 3세대 항생제는 C-6 위치에 F기를 도입한 것으로 연구의 진행 방향은 항균력의 향상과 체내에서의 지속 시간의 연장, 경구 투여시 흡수로의 증가와 독성의 약화를 위한 것이다. 본 연구는 quinolone의 기본 골격을 유지하면서 C-7 위치에 새로운 group을 도입하여 그에 대한 항균력을 측정하여 새로운 quinolone계 항생제의 개발을 시도하였다.

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Antibiotic Resistance of Staphylococcus Aureus (황색포도알균의 항생제 내성)

  • Kim, Yun-Kyung;Hong, Hae-Sook;Jeong, Jae-Sim
    • Journal of Korean Biological Nursing Science
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    • v.8 no.1
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    • pp.5-14
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    • 2006
  • Staphyloccus aureus is one of the most important pathogens in clinical settings. It is also one of the leading causes of nosocomial infections and the dissemination of multiple drug-resistant strains, mainly methicillin resistant Staphyloccus aureus, and the recent emergence of a vancomycin resistant MRSA is the concern to hospital worldwide. MRSA strains have acquired multiple resistance to a wide range of antibiotics, including aminoglycosides and macrolides. $\beta$-Lactam resistance of methicillin-resistnat Staphyococcus aureus is determined by the function of penicillin binding protein 2'(PBP2') encoded by the methicillin resistance gene mec A. MRSA strains carry methicillin resistance gene mecA, encoded by a mobile genetic element designated staphylococoal cassette chromosome mec(SCCmec). MRSA clones are defined by the type of SCCmec element and the genotype of the methicilline-susceptible Staphyococcus aureus chromosome in which the SCCmec element is integrated.

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A Study on the Microbiological Assay of Bacampicillin Hydrochloride (염산바캄피실린의 역가 검정법에 관한 연구)

  • Chung, Kyeong-Soo;Kim, Young-Jun;Lee, Song-Ae;Kim, Byung-Kak
    • The Korean Journal of Mycology
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    • v.8 no.1
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    • pp.69-71
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    • 1980
  • To establish a competent method of microbiological assay for bacampicillin, one of new semi-synthetic derivatives of ${\beta}-lactam$ antibiotics, a comparison was carried out between different conditions for hydrolysis of bacampicillin into ampicillin which was then subjected to cylinder plate method. The results showed that the use of carboxylic ester hydrolase in vitro as a pretreatment of it in either pH value 6 or 8 was feasible and that the cylinder plate method with Sarcina lutea was adequate for potency estimation.

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Isolation and Characterization of Soil Strains Producing Glutaryl-7-Aminocephalosporanic Acid Acylase

  • Knang, Yong-Ho;Yoo, Ryong-Hoon
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.2 no.2
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    • pp.105-108
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    • 1997
  • A search was undertaken to screen microorganisms that produce an enzyme capable of deacylating glutary1-7-amincephalosporanic acid to 7-aminocephalosporanic acid in soil samples. The screening was carried out by preparing enrichment cultures containing glutary-7ACA and cephalosporin C as selective carbon sources. A non-${\beta}$-lactam model compound,, glutary-p-nitroanilide, was synthesized as a substrate suitable for the rapid screening of microorganisms isolated from the enrichment cultures. Two isolates exhibiting acylase activity, designated BY7.4 and BY8.1, were identified as strains of Pseudomonas species. Pseudomonas BY8.1 showed higher acylase activity toward G1-7ACA than Pseudomonas BY7.4. Environmental conditions for the optimal acylase activity of Pseudomonas BY8.1 were shown to be pH9 and 30$^{\circ}C$.

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Antigenicity Study on IDC7181, a Quaternary Ammoniopropenyl Cephalosporin Possessing Two Vinyl Groups (Cephalosporin계 항생제 IDC7181에 대한 항원성시험)

  • 신지순;장호송;최은경;권운;채희열;조영민;김윤배;강종구
    • Toxicological Research
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    • v.19 no.4
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    • pp.321-324
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    • 2003
  • Antigenic potential of a novel cephalosporin, IDC7181 was examined a active systemic anaphylaxis (ASA) and passive cutaneous anaphylaxis (PCA) test, in guinea pig and mouse-rat models, respectively. In ASA test, IDC7181 induced the signs of restlessness in a few animals immunized with a high dose (100 mg/kg) of IDC7181 alone or in combination with Freund's complete adjuvant (FCA). In PCA test, only one of ten sera from the animals immunized with a high dose (100 mg/kg) of IDC7181 in the absence or presence of FCA showed positive reaction. The positive reaction, induced by IDC7181, which may be due to $\beta$-lactam ring, in ASA and PCA tests were negligible in comparison with those of traditional cephalosporins. Taken together, it is suggested that IDC7181 do not cause immunological problems in clinical dosage.

Classification of Bacteroides Fragilis Group (Bacteroides Fragilis군의 분리 및 동정에 관하여)

  • Kim, Hee-Sun
    • The Journal of the Korean Society for Microbiology
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    • v.21 no.4
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    • pp.481-485
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    • 1986
  • Six strains of Bacteroides fragilis group were isolated from clinical specimens, and these isolates were classified by the resistance to bile and kanamycin, and by catalase and indole reaction. Of 6 strains, 4 strains were belonged to B. fragilis and 2 were B. uniformis. Among 6 strains, only 2 of B. fragilis harbored plasmids. But these plasmid showed no correlation with phenotypic expression. There were some differences in susceptibility to 23 ${\beta}$-lactam antibiotics, also, marked susceptibility differences were found between 2 species, so these results may be contributed to the treatment of infection due to this micro-organism and the identification of these species.

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Comparison of residual antibiotic materials in meet -Slaughtered cattle and swine in Seoul- (식육중 잔류항균물질 비교 조사 -서울지역 도축 소와 돼지를 중심으로-)

  • 변정옥;강영일;이달주;황래홍;이양수;이병동
    • Korean Journal of Veterinary Service
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    • v.25 no.3
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    • pp.229-236
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    • 2002
  • This study was carried out to compare the residual antibiotic materials in muscles of slaughter cattle and swine from slaughterhouses in Seoul from 2000 to 2001 by EEC-4-plate method, Charm II and HPLC method. 1. Residual antibiotic materials were detected from 95 samples(0.8%) by EEC-4-plate and 57 samples(10.2%) by Charm II. The final HPLC method determined the positives are 43(45.3%) and 27(47.3%) respectively. 2. The detection ratios were 45% by EEC-4-plate and 47% by Charm II. 3. Seventy samples were classified as tetracyclines 56(75.7.4%), sulfonamides 10(14.9%), $\beta$-lactam 6(8.1%) chloramphenicol 1(1.4%). Three of them were confirmed to be positive simmultaneously for tetracyclines, sulfonamides and chloramphenicol. 4. The highest residual concentration of chlortetracycline, oxytetracycline, sulfamethazine, sulfadimethoxine, sulfaquinoxaline, penicillin, ampicillin and chloramphenicol were 0.34, 11.29, 68.16, 0.13, 4.0, 0.12, 0.4 and 0.04ppm, respectively.

Total Synthesis of Sodium (3S,4R)-3-[2-(2-Aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-4-methoxymethyl-2-azetidinone-1-sulfonate from D-Aspartic Acid

  • Chung Bong Young;Kim, Jin Yeon;Nah Cha Soo;Han Kee Jong;Park, Jong Ok
    • Bulletin of the Korean Chemical Society
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    • v.13 no.3
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    • pp.315-316
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    • 1992
  • Sodium (3S,4R)-3-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyi minoacetamido]-4-methoxymethyl-2-azetidinone-1- sulfonate (2) was synthesized in fourteen steps from D-aspartic acid. Starting from D-aspartic acid, (3S,4R)-3-amino-1-t-butyldimethylsilyl-4-methoxym ethyl-2-azetidinone (12) was synthesized in ten steps. Acylation of the amino group of 12 with $2-amino-{\alpha}-(methoxyimino)-4-thiazoleacetic$ acid, desilylation, sulfonation, and ion exchange afforded sodium (3S,4R)-3-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyi minoacetamido]-4-methoxymethyl-2-azetidinone-1- sulfonate (2). This new ${\beta}-lactam$ compound 2 showed low antibacterial activities.

Clinical Significance of Extended-Spectrum ${\beta}$-Lactamase Producing $Escherichia$ $coli$ in Pediatric Patients with Febrile Urinary Tract Infection (발열성 소아 요로감염에서 Extended-Spectrum ${\beta}$-Lactamase 생성 $Escherichia$ $coli$의 임상적 의의)

  • Park, Cheol;Kim, Min-Sang;Kim, Mi-Kyung;Yim, Hyung-Eun;Yoo, Kee-Hwan;Hong, Young-Sook;Lee, Joo-Won
    • Childhood Kidney Diseases
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    • v.16 no.1
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    • pp.38-45
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    • 2012
  • Purpose: The incidence of community-acquired urinary tract infection (UTI) due to extended-spectrum ${\beta}$-lactamase producing $Escherichia$ $coli$ (ESBL(+) $E.$ $coli$) has increased worldwide. ESBL causes resistance to various types of the newer ${\beta}$-lactam antibiotics, including the expanded spectrum cephalosporins and monobactams. We aimed to investigate the severity of UTI and associated genitourinary malformations in children with febrile UTI caused by ESBL(+) $E.$ $coli$. Methods: We retrospectively reviewed the medical records of 290 patients diagnosed as febrile UTI caused by $E.$ $coli$ between January 2008 and October 2010 at Korea University Medical center. We classified the patients into two groups with ESBL(+) and ESBL(-) $E.$ $coli$ group according to the sensitivity of urine culture. Fever duration, admission period, white blood cell (WBC) counts and C-reactive protein (CRP) in peripheral blood, the presence of hydronephrosis, cortical defects, vesicoureteral reflux (VUR) and renal scar were compared between the two groups. Results: Patients with ESBL(+) $E.$ $coli$ were 32, and those with ESBL(-) $E.$ $coli$ were 258. If we excluded those tested with a sterile urine bag, patients with ESBL(+) $E.$ $coli$ were 22, and those with ESBL(-) $E.$ $coli$ were 212. Whether the results of sterile urine bag tests were included or not, there was no significant difference in all parameters between the two groups statistically. Conclusion: Our data shows that ESBL(+) $E.$ $coli$ may not be related to the severity of UTI and associated genitourinary malformations.

A Fifteen-year Epidemiological Study of Ventriculoperitoneal Shunt Infections in Pediatric Patients: A Single Center Experience (소아 환자에서의 뇌실-복강 단락 감염의 역학적 고찰: 15년 간의 단일 기관 연구)

  • Kim, Yeon Kyung;Shin, Hyung Jin;Kim, Yae Jean
    • Pediatric Infection and Vaccine
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    • v.19 no.3
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    • pp.141-148
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    • 2012
  • Purpose : Ventriculoperitoneal (VP) shunt insertion is an important treatment modality in children with hydrocephalus. VP shunt infection is a major complication and an important factor that determines the surgery outcome. This 15-year study was performed to evaluate the epidemiology of VP shunt infections in pediatric patients treated at our center. Methods : A retrospective review of medical records was performed in patients 18 years old or younger who underwent VP shunt insertion surgery from April 1995 to June 2010. Results : Three hundred twenty-seven VP shunt surgeries were performed in a total of 190 pediatric patients (83 females, 107 males). The median age of the patients was 2.4 years (range, 0.02-17.9 years). Having a malignant brain tumor was the most frequent cause for VP shunt insertion. The shunt infection rate was 6.7% (22/327) per 100 operations and 9.5% (18/190) per 100 patients, and the incidence rate was 0.45 infection cases per 100 shunt operations-year. The most common pathogen was coagulase-negative staphylococcus (n=7) followed by methicillin resistant Staphylococcus aureus (n=1). Ten cases were treated with vancomycin and beta-lactam antibiotic (cephalosporin or carbapenem) combination therapy and 7 cases were treated with vancomycin monotherapy. The median duration of antibiotic treatment was 26 days (range, 7 to 58 days). Surgical intervention was performed in 18 cases (18/22, 81.8%). Conclusion : Epidemiologic information regarding VP shunt infections in pediatric patients is valuable that will help guide proper antibiotic management. Additional studies on the risk factors for developing VP shunt infections are also warranted.

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