• Title/Summary/Keyword: Cephalosporins

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Synthesis and Biological Evaluation of New Aminothiazolyl Cephalosporins with Elongated Side Chains

  • Kang, Han-Young;Koh, Hun-Yeong;Kim, Mi-Young;Kim, Hyun-Mi;Yoon, Du-Weon;Chang, Moon-Ho
    • Bulletin of the Korean Chemical Society
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    • v.12 no.6
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    • pp.666-673
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    • 1991
  • The elongation of the chain length at 2'position of aminothiazolylacetamido group of cephalosporin antibiotics was achieved. The derivatives with elongated side chain at 2'position were successfully synthesis and their in vitro activities were evaluated. It is indicated that there is an optimum range of the chain length in order to exhibit higher biological activities. This result could open a possibility for the development of the cephalosporin antibiotics with higher activities by further variation of the substituents at other positions. The cephalosporin derivatives with a simple (relatively non-functionalized) side chain as well as with a linear extended side chain were also prepared. Low activities of these derivatives led to a conclusion that either simple (non-functionalized) change or linear elongation of the side chain does not enhance the antibacterial activities.

An Effective Acylation of Cephalosporins Using 1-Methanesulfonyloxy-6-trifluoromethylbenzotriazole$^\dag$

  • Lee, Cheol-Hae;Moon, Chi-Jang;Kim, Kyeong-Sook;Kim, Jae-Hak;Kim, Dae-Whang
    • Bulletin of the Korean Chemical Society
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    • v.8 no.4
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    • pp.336-338
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    • 1987
  • A new coupling agent, 1-methanesulfonyloxy-6-trifluoromethyl-benzotriazole (3), was prepared by the reaction of 1-hydroxy-6-trifluoromethylbenzotriazole (1) and methanesulfonyl chloride. 3 was reacted with 2-(2-amino-4-thiazolyl)-2-synalkoxyi minoacetic acid (4) to give a mixture of active intermediates (5 and 6), which was treated with 7-aminocephalosporanic acid derivatives (10) to afford cephalosporin derivatives (11) in short reaction time with high yields.

Urinary Tract Infection in Febrile Infants with Pyuria (발열과 농뇨가 있는 영아에서 요로감염에 관한 연구)

  • Lee, Sue Young;Cho, Sung Hee;Kim, Sun Mi;Jeong, Dae Chul;Chung, Seung Yeon;Lee, Kyung Yil;Kang, Jin Han
    • Pediatric Infection and Vaccine
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    • v.11 no.1
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    • pp.90-100
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    • 2004
  • Objective : Urinary tract infection(UTI) is a frequent serious bacterial infection in young infants. The clinical presentation may be non-specific and variable, depends on factors such as the age and the level of infection. Children with renal involvement may be at risk of permanent renal damage. Experimental studies have shown that renal lesions caused by acute febrile UTI may be prevented or diminished by early diagnosis and treatment. Therefore, it is important to find a method that can permit early diagnosis and identification of patients who are at risk for progressive renal damage. We designed this study to identify related factors in culture positive UTI infants, and also to identify related factors in culture negative UTI infants, who are febrile with pyuria, by using renal imaging and functional studies including renal sonography, DMSA scan and VCUG. Methods : Retrospectively analyzed the medical records of 136 febrile infants with pyuria over 2 years(from January 2001 to February 2003). Urine culture was done in all cases, and regardless of urine culture findings, renal imaging study was done if symptomatic UTI suspected. Results : Total 57 organisms were isolated in 53 patients. E. coli was the most common organism(86%), followed by E. faecalis, M. morganii, Proteus species, P. aeruginosa, S. aureus and E. fergusonii. Most of the isolates had high sensitivity on cephalosporins or amikacin and had low sensitivities on aminopenicillins. Abnormal acute phase DMSA scan or VCUG findings were seen in both urine culture positive and negative group without statistical differences(P>0.05). In febrile infants with pyuria, fever over 48 hours, older age and high CRP related to abnormal acute phase DMSA scan findings regardless urine culture results. Conclusion : 1st or 3rd generation cephalosporins with amikacin could be the first choice of treatment for UTI. Febrile infants with positive urine culture dose mean urinary tract infection but not acute pyelonephritis which directly relates to cortical damage which could be confirmed by acute phase DMSA scan. Even cases with negative urine culture findings, acute pyelonephritis should be concerned in febrile infants with pyuria who are older than 3 months of age, has fever over 48 hours or high CRP level. And in such cases, acute phase DMSA scan and VCUG should be evaluated for early treatment and long term prognosis.

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The Antibiotic Resistance Pattern of Gram-Negative Bacteria in Children Younger Than 24 Months with a Urinary Tract Infection: A Retrospective Single-Center Study over 15 Consecutive Years

  • Lee, Yoon Kyoung;Lee, Haejeong;Kim, Jong Min;Kang, Ji-Man;Lee, Sang Taek;Lee, Nam Yong;Kim, Yae-Jean;Cho, Heeyeon
    • Childhood Kidney Diseases
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    • v.19 no.2
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    • pp.148-153
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    • 2015
  • Purpose: We investigated trends in antibiotic resistance for gram-negative bacteria in infants with a urinary tract infection (UTI) over 15 years at a single institution. Methods: A retrospective chart review was conducted for children younger than 24 months who visited the emergency room and were diagnosed with a UTI between January 2000 and December 2014. We selected urine culture data that grew Escherichia coli and Klebsiella pneumoniae. Baseline clinical information and results of antimicrobial susceptibility tests were analyzed by dividing the 15-year study time frame into three periods (A: 2000-2004, B: 2005-2009, and C: 2010-2014). Results: During the study period, 478 applicable children were identified (E. coli, 89.7% and K. pneumoniae, 10.3%). Antibiotic resistance to third-generation cephalosporins was increased from period A to period C (A, 2.1%; B, 8.3%; C, 8.8%; P=0.025). Resistance to quinolones also showed a steady pattern during periods A to C, although it was not statistically significant (A, 7.9%; B, 9.7%; C, 12.4%; P=0.221). The incidence of Extended-spectrum ${\beta}$-lactamase (ESBL)-producing gram-negative bacteria increased from period A to period C (A, 1.4%; B, 7.6%; C, 8.2%; P=0.012). Conclusion: This study revealed that the common uropathogens E. coli and K. pneumoniae experienced increasing resistance rates against third-generation cephalosporins and a constant antibiotic resistance to quinolones in children younger than 24 months. We also showed a recent increased incidence of ESBL-producing gram-negative bacteria in patients with community-acquired UTIs. Therefore, it is necessary to actively surveil resistance in order to properly select empirical antibiotics.

Impact of antimicrobial resistance in the $21^{st}$ century

  • Song, Jae-Hoon
    • Proceedings of the Korean Society for Applied Microbiology Conference
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    • 2000.04a
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    • pp.3-6
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    • 2000
  • Antimicrobial resistance has been a well-recognized problem ever since the introduction of penicillin into clinical use. History of antimicrobial development can be categorized based on the major antibiotics that had been developed against emerging resistant $pathogens^1$. In the first period from 1940 to 1960, penicillin was a dominating antibiotic called as a "magic bullet", although S.aureus armed with penicillinase led antimicrobial era to the second period in 1960s and 1970s. The second stage was characterized by broad-spectrum penicillins and early generation cephalosporins. During this period, nosocomial infections due to gram-negative bacilli became more prevalent, while those caused by S.aureus declined. A variety of new antimicrobial agents with distinct mechanism of action including new generation cephalosporins, monobactams, carbapenems, ${\beta}$-lactamase inhibitors, and quinolones characterized the third period from 1980s to 1990s. However, extensive use of wide variety of antibiotics in the community and hospitals has fueled the crisis in emerging antimicrobial resistance. Newly appeared drug-resistant Streptococcus pneumoniae (DRSP), vancomycin-resistant enterococci (VRE), extended-spectrum ${\beta}$-lactamase-producing Klebsiella, and VRSA have posed a serious threat in many parts of the world. Given the recent epidemiology of antimicrobial resistance and its clinical impact, there is no greater challenge related to emerging infections than the emergence of antibiotic resistance. Problems of antimicrobial resistance can be amplified by the fact that resistant clones or genes can spread within or between the species as well as to geographically distant areas which leads to a global concern$^2$. Antimicrobial resistance is primarily generated and promoted by increased use of antimicrobial agents. Unfortunately, as many as 50 % of prescriptions for antibiotics are reported to be inappropriate$^3$. Injudicious use of antibiotics even for viral upper respiratory infections is a universal phenomenon in every part of the world. The use of large quantities of antibiotics in the animal health industry and farming is another major factor contributing to selection of antibiotic resistance. In addition to these background factors, the tremendous increase in the immunocompromised hosts, popular use of invasive medical interventions, and increase in travel and mixing of human populations are contributing to the resurgence and spread of antimicrobial resistance$^4$. Antimicrobial resistance has critical impact on modem medicine both in clinical and economic aspect. Patients with previously treatable infections may have fatal outcome due to therapeutic failure that is unusual event no more. The potential economic impact of antimicrobial resistance is actually uncountable. With the increase in the problems of resistant organisms in the 21st century, however, additional health care costs for this problem must be enormously increasing.

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First Detection of $bla_{IMP-1}$ in Clinical Isolate Multiresistant Acinetobacter baumannii from Korea

  • Jeong Seok-Hoon;Bae Il-Kwon;Sohn Seung-Ghyu;Park Kwang-Ok;An Young-Jun;Sung Kwang-Hoon;Jang Seon-Ju;Heo Myong-Jin;Yang Ki-Suk;Lee Sang-Hee
    • Journal of Microbiology and Biotechnology
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    • v.16 no.9
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    • pp.1377-1383
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    • 2006
  • Among 46 Acinetobacter baumannii isolates collected in 2004, two imipenem-resistant isolates were obtained from clinical specimens taken from patients hospitalized in Busan, Republic of Korea. Two carbapenemase-producing isolates were further investigated to determine the mechanism of resistance. These isolates were analyzed by antibiotic susceptibility testing, microbiological tests of carbapenemase activity, determination of pI, transconjugation test, enterobacterial repetitive consensus (ERIC)-PCR, and DNA sequencing. Two cases of infection by A. baumannii producing the IMP-1 ${\beta}$-lactamase were detected. The isolates were characterized by a modified cloverleaf synergy test and EDTA-disk synergy test. Isoelectric focusing of crude bacterial extracts revealed nitrocefin-positive bands with a pI value of 9.0. PCR amplification and characterization of the amplicons by direct sequencing indicated that the isolates carried a $bla_{IMP-l}$ determinant. The isolates were characterized by a multidrug resistance phenotype, including penicillins, extended-spectrum cephalosporins, carbapenems, and aminoglycosides. These results indicate that the observed imipenem resistance of two Korean A. baumannii isolates was due to the spread of an IMP-1-producing clone. Our microbiological test of carbapenemase activity is simple to screen class B metallo-${\beta}$-lactamase-producing clinical isolates to determine their clinical impact and to prevent further spread. This study shows that the $bla_{IMP-l}$ resistance determinant, which is emerging in Korea, may become an emerging therapeutic problem, since clinicians are advised not to use extended-spectrum cephalosporins, imipenem, and aminoglycosides. This observation emphasizes the importance of having effective control measures in Asian hospitals, such as early detection of colonized patients, isolation procedures, and a judicious use of antibiotics.

Genotypic Detection of Extended-Spectrum β-Lactamase-Producing of Klebsiella pneumoniae (Extended-Spectrum β-Lactamase 생성 Klebsiella pneumoniae 균주의 유전형 검출)

  • Yook, Keun-Dol;Yang, Byoung-Seon;Park, Jin-Sook
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.14 no.3
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    • pp.1191-1196
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    • 2013
  • Among Gram-negative pathogens in Korea, the incidence of resistance to third generation cephalosporins is becoming an ever-increasing problem. The production of extended-spectrum ${\beta}$-lactamase (ESBL) is the main mechanism of bacterial resistance to a third-generation cephalosporins and monobactams. Accurate identification of the ESBL genes are necessary for surveillance and epidemiological studies of the mode of transmission in the hospital. This study was conducted to detect the genes encoding ESBL of 46 K. penumoniae isolated from Daejeon, Chungnam and Chungbuk regional university hospitals from February to August in 2012. The phenotypes of the isolated specimens were examined according to the combination disc test (CDT) by the Clinical and Laboratory Standards Institute (CLSI). Forty two ESBL producing K. penumoniae isolates could be detected using ceftazidime (CAZ) discs with and without clavulanate (CLA). By CDT, 42 K. pneumoniae strains were confirmed to be ESBL strains. Genotyping was performed by multiplex PCR with type-specific primers. By PCR analysis, TEM gene in 46 strains, SHV gene in 37 strains and CTX-M genes in 14 strains were identified. Ten isolates did carry genes encoding ESBLs of all types TEM, SHV and CTX-M. The multiplex polymerase chain reaction (PCR) analysis was better to detect and differentiate ESBL producing K. penumoniae strains in clinical isolates.

Classification of Critically Important Antimicrobials and their Use in Food Safety (중요 항생제의 분류와 식품안전분야에서 활용)

  • Hyo-Sun Kwak;Jun-Hyeok Ham;Eiseul Kim;Yinhua Cai;Sang-Hee Jeong;Hae-Yeong Kim
    • Journal of Food Hygiene and Safety
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    • v.38 no.4
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    • pp.193-201
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    • 2023
  • Antimicrobials in human medicine are classified by The World Health Organization (WHO) into three groups: critically important antimicrobials (CIA), highly important antimicrobials (HIA), and important antimicrobials (IA). CIA are antibiotic classes that satisfy two main criteria: that they are the sole or the only available limited therapeutic option to effectively treat severe bacterial infections in humans (Criterion 1), and infections where bacteria are transmitted to humans from non-human sources or have the potential to acquire resistance genes from non-human sources (Criterion 2). WHO emphasizes the need for cautious and responsible use of the CIA to mitigate risk and safeguard human health. Specific antimicrobials within the CIA with a high priority for management are reclassified as "highest priority critically important antimicrobials (HP-CIA)" and include the 3rd generation of cephalosporins and the next generation of macrolides, quinolones, glycopeptides, and polymyxins. The CIA list is the scientific basis for risk assessment and risk management policies that warrant using antimicrobials to reduce antimicrobial resistance in several countries. In addition, the CIA list ensures food safety in the food industry, including for the popular food chain companies McDonald's and KFC. The continuous update of the CIA list reflects the advancement in research and emerging future challenges. Thus, active and deliberate evaluation of antimicrobial resistance and the construction of a list that reflects the specific circumstances of a country are essential to safeguarding food security.

Prescription of antibiotics after tooth extraction in adults: a nationwide study in Korea

  • Choi, Yoon-Young
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.46 no.1
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    • pp.49-57
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    • 2020
  • Objectives: This study aimed to understand the nationwide patterns of antibiotic prescription after tooth extraction in adult patients. Materials and Methods: This study analyzed dental records from the National Health Insurance Service-National Sample Cohort (NHIS-NSC) database on 503,725 tooth extractions performed in adults (≥19 years) during 2011-2015. Patient sex, age, household income, systemic disease (diabetes mellitus and hypertension), type of dental institution, region of dental institution, year of prescription, and type of tooth extraction procedure were considered. The antibiotic prescription rate and broad-spectrum antibiotic prescription frequency were analyzed using chi-squared tests. Factors affecting the prescription of broad-spectrum antibiotics were evaluated using multivariate logistic regression analysis. Results: The rate of antibiotic prescription after tooth extraction was 81.85%. Penicillin was most commonly prescribed (45.25%), followed by penicillin with beta-lactamase inhibitors (18.76%), metronidazole (12.29%), and second- to fourth-generation cephalosporins (11.52%). The proportion of broad-spectrum antibiotics used among all prescribed antibiotics was 45.88%. Conclusion: The findings of this study demonstrate that the rate of antibiotic prescription after tooth extraction is higher in Korea than in other countries. Furthermore, broad-spectrum antibiotics are used more frequently, which may indicate unnecessary drug prescription, an important contributor to antibiotic resistance.

Listeria Species in Broiler Poultry Farms: Potential Public Health Hazards

  • Dahshan, Hesham;Merwad, Abdallah Mohamed Amin;Mohamed, Taisir Saber
    • Journal of Microbiology and Biotechnology
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    • v.26 no.9
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    • pp.1551-1556
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    • 2016
  • Broiler meat production worldwide has been plagued by lethal food-poisoning bacteria diseases, including listeriosis. A fatality rate of 15.6% was recorded in human beings in the EU in 2015. During 2013, a total of 200 poultry farm samples, including litter, chicken breast, farm feed, and drinking water, were collected to generate baseline data for the characterization of the genus Listeria in broiler poultry farms. Listeria spp. were detected in a total of 95 (47.5%) poultry farm samples. The isolates of Listeria spp. included L. innocua (28.5%), L. ivanovii (12.5%), L. welshimeri (4.5%), and L. monocytogenes and L. seeligeri (1% each). Listeria spp. contamination rates were higher in farm feed (70%), followed by litter (52.5%), chicken breasts (42.2%), and drinking water (10%). Almost all Listeria spp. isolates were resistant to more than three classes of antibiotics (multidrug resistant). Besides this, we observed a significant resistance level to penicillin and fluoroquinolone drugs. However, lower resistance levels were recorded for broad-spectrum cephalosporins. The inlA, inlC, and inlJ virulence genes were detected in almost all of the L. monocytogenes isolates. Thus, food safety management approaches and interventions at all stages of the broiler rearing cycle were needed to control cross-contamination and the zoonotic potential of listeriosis.