• Title/Summary/Keyword: 베타-락탐 항생제

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신규베타락탐계 항생제 합성과 항균성

  • 고옥현;김경수;하재천;고봉석
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.171-171
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    • 1994
  • Cephem ring의 C-7위치에 aminothiazoly lmethoxyimino기를 가진 화합물들이 항균활성을 증가시키고, G(-)균의 외막투과성을 촉진시킬뿐 아니라 광범위항균 spectrum을 갖게 하고 $\beta$-lactamase에 안정하며 PBP(penicillin binding protein)에 대한 결합친화성을 증가시킨다는 보고에 따라 본 저자는 C-7위치에 cefotaxime구조와 같이 aminothiazolylmethoxyimino acetamido moiety를 고정시키고 항균활성을 증가시키기 위하여 약리활성이 기대되는 5-(substituted)-2H-tetrazole유도체들을 합성하여 C-3 위치에 도입시킨 새로운 화합물 7$\beta$-〔(z)-2-(2-aminothiazol-4-yl)-2_(methoxyimino)acetamido〕-3-〔5-(substituted)tetrazol-2-yl〕 methyl-3-cephem-4-carboxylic acid 유도체를 합성하여 B. subtilis ATCC 6633, M. luteus ATCC 1004, E. coli KCTC 1039, E. coli ESS, K. pncumonia KCTC 1560, P. aeruginosa IF0 13130, S. typhimurium KCTC 1925, S. typhimurium SL 1102, 및 C. albicans ATCC 10231 등의 균과 fungus에 대하여 기존의 cefotaxime과 cefazoline을 대조물질로 사용하여 항균력을 비교하였다. 이들 화합물들은 대체적으로 M. luteus ATCC 6633, E. coli ESS, S. typhimurium SL 1102 균에 대해서는 cefotaxime보다 항균력이 우수하였으나 P. aeruginosa IF0 13130에 대해서는 항균력이 저하되었고 cefazolin보다는 대체적으로 항균력이 우수하였다.

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Synthesis of $\beta$-Lactam Antibiotics and Their Antibacterial Activity (베타 락탐계 항생제의 합성 및 항균력)

  • 홍석기;남재우;이경태;신관석
    • YAKHAK HOEJI
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    • v.37 no.2
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    • pp.158-162
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    • 1993
  • 6$\beta$-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl)acetamidopenicillanic acid(7a~7c) and 7$\beta$-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl) acetamidocephalosporanic acid(8a~8c) were synthesized and tested in vitro antibacterial activity. Of these new penicillins exhibited good antibacterial activity against Gram-positive bacteria whereas none of the compounds possessed the activity against Gram-negative bacteria at the concentration tested.

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Simultaneous analysis of β-lactam antibiotics and β-blockers by LC-MS/MS (LC-MS/MS를 이용한 베타락탐계 항생제와 베타차단제의 동시분석)

  • Son, Bo-young;Kim, Jun-il;An, Chi-hwa;Lee, Su-won;Kim, Bogsoon;Chung, Deukmo
    • Analytical Science and Technology
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    • v.29 no.4
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    • pp.179-185
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    • 2016
  • An effective analytical method has been developed for the determination of β-blockers(atenolol, metoprolol and propranolol) and 6 β-lactams(amoxicillin, penicillin G, cefaclor, cefadroxil, cephalexin and cephradine) in water samples using two different cartridges. The samples were extracted by solid-phase extraction (SPE) with the usage of polymeric hydrophile-lipophile balance(HLB cartridges) and strong cation-exchange mixed-mode polymeric sorbent (MCX cartridges). A XDB-C18 column(1.8 μm; 3.0 mm × 100 mm) was used for the sufficient chromatographic resolution. The calibration curves showed good linearity with high correlation coefficients (>0.995). The method detection limits (MDL) and the limits of quantification(LOQ) were from 1.1 to 3.9 ng/L and from 5 to 13 ng/L, respectively. The method was applied for the determination of the target compounds in tributaries and raw water of the Han River and these were found at N.D. to 0.209 μg/L.

Studies on the Synthesis and Antibacterial Activity of New $\beta$-Lactam Antibiotics (새로운 베타락탐 항생물질의 합성과 생물활성에 관한 연구)

  • Tae Heung Song;Young Ho Kim
    • Journal of the Korean Chemical Society
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    • v.36 no.2
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    • pp.293-300
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    • 1992
  • The synthesis of a series of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyiminoacetamido]-3-(4,6-diamino-1-alkyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylates is described. Variations of an oxyimino moiety in the 7-side chain and quaternary ammonium moiety in the 3-side chain were examined and structure-activity relationship was studied. The 4,6-diamino-1-methyl-1,3,5-triazinium-2-yl derivative of the 7-$\alpha$-methoxyimino series of cephalospoins, particularly 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido]-3-(4,6-diamino-1-methyl-1,3,5-triazinium-2-yl)thiomethyl-3-cephem-4-carboxylate(C-1), exhibited broad antibacterial activity against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.

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Non-carbapenem Drugs for Patients with Bacteremia caused by Extended-Spectrum β-Lactamase-Producing Enterobacteriaceae: Piperacillin-Tazobactam (Extended-Spectrum β-Lactamase 생성 장내세균속균종 균혈증 환자들의 치료에서 비카바페넴 항생제의 단일 기관 치료 결과: Piperacillin-Tazobactam을 중점으로)

  • Hyunjoo Oh;Seunghee Lee;Misun Kim;Sang Taek Heo;Jeong Rae Yoo
    • The Korean Journal of Medicine
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    • v.99 no.3
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    • pp.149-157
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    • 2024
  • Background/Aims: Carbapenems are recommended for treating bacteremia caused by extended-spectrum β-lactamase (ESBL) producing Enterobacteriaceae (ESBL-E). However, this has resulted in a significant rise in the utilization of carbapenems in cases of ESBL-E infection. We evaluated the clinical outcomes of patients with ESBL-E bacteremia treated with non-carbapenem antimicrobials. Methods: We conducted a retrospective case-control study of a cohort of patients with documented ESBL-E bacteremia from January 2021 to December 2021. The patients were divided into two groups according to whether they received non-carbapenem or carbapenem therapy. The rates of treatment failure, 30-day mortality and microbiologic failure, and the durations of hospitalization and of antimicrobial therapy were compared between the two groups. Antimicrobial susceptibility testing and phenotypic identification of ESBL-E were performed using the Vitek 2 system. Results: Of 118 patients with ESBL-E bacteremia, 54 received non-carbapenem drugs (non-carbapenem group [NCG]) and 64 received carbapenems (carbapenem group [CG]). Treatment failure at 30 days occurred in 16.7% of the patients in the NCG and in 18.8% in the CG (p = 0.65). The 30-day mortality rate was 14.8% in the NCG and 17.2% in the CG (p = 0.63). Extra-urinary tract infection and prior antimicrobial therapy within 30 days were risk factors for treatment failure in patients with ESBL-E bacteremia. The clinical outcomes did not differ significantly between the two groups, challenging the prevailing preference for carbapenems in the treatment of ESBL-E bacteremia. Conclusions: Non-carbapenem antimicrobials such as piperacillin/tazobactam are recommended for patients with mild ESBL-E bacteremia in South Korea.

Complete genome sequence of Salmonella Thompson strain MFDS1004024 isolated from crab-stick (게맛살에서 분리된 Salmonella Thompson MFDS1004024의 유전체 염기서열 분석)

  • Park, Sewook;Lee, Woojung;Yoo, Ran Hee;Joo, In-Sun;Kwak, Hyo Sun;Kim, Soon Han
    • Korean Journal of Microbiology
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    • v.54 no.2
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    • pp.155-157
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    • 2018
  • Salmonella enterica subsp. enterica serovar Thompson strain MFDS1004024 was isolated from crab-stick in Korean food-borne outbreak in 2014. Here, we present the complete genome sequence of strain MFDS1004024 with a size of 4,742,942 bp and a mean G + C content of 52%. The genome included 4,373 coding sequences, and 22 ribosomal RNA and 84 transfer RNA genes. Also, we found that strain MFDS1004024 has some genes for Salmonella infection and beta-lactam resistance in its genome based on the result of genome analysis.

Interaction with Polyphenols and Antibiotics (폴리페놀 화합물과 항생제의 상호작용)

  • Cho, Ji Jong;Kim, Hye Soo;Kim, Chul Hwan;Cho, Soo Jeong
    • Journal of Life Science
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    • v.27 no.4
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    • pp.476-481
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    • 2017
  • Polyphenols are secondary metabolites produced by higher plants and have been used as antiallergic, anticancer, antihypertensive, antiinflammatory, antimicrobial and antioxidant agents. They are generally divided into flavonoids and non-flavonoids. The antimicrobial activity of flavonoids are stronger than that of non-flavonoids. The skeleton structures of flavonoids possessing antimicrobial activity are chalcone, flavan-3-ol (catechin), flavanone, flavone, flavonol and proanthocyanidin. The flavonols are shown antibacterial activity against several gram-positive bacteria (Actinomyces naeslundii, Lactobacillus acidophilus and Staphylococcus aureus) and gram-negative bacteria (Fusobacterium nucleatum, Porphyromonas gingivalis, Prevotella melaninogenica and Prevotella oralis). Among of non-flavonoids, caffeic acids, ferulic acids and gallic acids showed antimicrobial activity against gram-positive (Listeria monocytogenes and S. aureus) and gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). These are found to be more efficient against the E. coli, L. monocytogenes, P. aeruginosa and S. aureus than antibiotics such as gentamicin and streptomycin. The kaempferol and quercetin showed synergistic effect with ciprofloxacin and rifampicin against S. aureus and methicillin resistant S. aureus (MRSA). Epigallocatechin gallate (EGCG) acts synergistically with various ${\beta}-lactam$ antibiotics against MRSA. In particular, the epicatechin, epigallocatechin (EGC), EGCG and gallocatechin gallate from Korean green tea has antibacterial activity against MRSA clinical isolates and the combination of tea polyphenols and oxacillin was synergistic for all the clinical MRSA isolates.

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.

Treatment of Multidrug-resistant Pseudomonas aeruginosa Bacteremia in a Immunocompromised Child With Ceftolozane-tazobactam (면역저하 소아에서 발생한 다제내성 녹농균 균혈증을 ceftolozane-tazobactam으로 성공적으로 치료한 증례보고)

  • Hyesun Yu;Areum Shin;Doo Ri Kim;Jaeyoung Choi;Hee Young Ju;Joongbum Cho;Cheol-In Kang;Yae-Jean Kim
    • Pediatric Infection and Vaccine
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    • v.30 no.1
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    • pp.47-54
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    • 2023
  • With the widespread use of broad-spectrum antibiotics in clinical practice, the emergence of multidrug-resistant (MDR) gram-negative bacteria has become a global problem. The MDR Pseudomonas aeruginosa infection is especially difficult to treat and increases mortality in critically ill patients. Ceftolozane-tazobactam (ZerbaxaTM) is a fifth-generation cephalosporin and beta-lactamase inhibitor that has proved to be effective for treating complicated urinary tract infections and complicated intra-abdominal infections caused by MDR P. aeruginosa. Herein, we report the first case of pediatric hematologic cancer in Korea that was successfully treated for MDR P. aeruginosa bacteremia with Ceftolozane-tazobactam.

Stenotrophomonas maltophilia and Ventilator-Associated Pneumonia in Critically Ill Pediatric Patients: a Retrospective Analysis at a Single Center (소아 환자에서 Stenotrophomonas maltophilia와 인공 환기요법 관련 폐렴에 관한 연구)

  • Lee, Byung-Kee;Choi, Soo-Han;Kim, Soo Jin;Cho, Joong Bum;Ae, Hong;Yoo, So-young;Kim, Ji Hye;Lee, Nam Young;Kim, Yae-Jean
    • Pediatric Infection and Vaccine
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    • v.22 no.2
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    • pp.75-80
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    • 2015
  • Purpose: Ventilator-associated pneumonia (VAP) is a serious threat in critically ill pediatric patients. Data regarding Stenotrophomonas maltophilia VAP in pediatric population is limited. We evaluated the clinical data of S. maltophilia associated VAP in critically ill pediatric patients. Methods: A retrospective chart review was performed in pediatric patients 18 years old or younger who developed S. maltophilia associated VAP at Samsung Medical Center, Seoul Korea from January 2008 to December 2012. Results: A total of 31 patients were identified S. maltophilia associated VAP. Median age was 8 months (range, 0.5 month to 16.6 years) and 13 patients were male (40.6%). Underlying illnesses were cardiologic diseases (n=11, 34.4%), hematologic oncologic malignancies (n=7, 25%), neurologic diseases (n=4, 12.5%), pulmonary diseases (n=3, 9.4%), and others (n=4, 12.5%). The median duration of ventilator use before S. maltophilia VAP diagnosis was 14 days (range, 4-256 days). Overall mortality at 30 days was 12.5% (4/32). Conclusions: S. maltophilia should be also considered as a possible pathogen for VAP in critically ill pediatric patients. Empiric antibiotic choice should include agents that are active against S. maltophilia in patients who are deteriorating on broad spectrum beta-lactam antimicrobial agents.