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beta-lactamase inhibitor

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https://www.readbyqxmd.com/read/27951476/a-nitrocefin-based-amperometric-assay-for-the-rapid-quantification-of-extended-spectrum-%C3%AE-lactamase-producing-escherichia-coli-in-wastewaters
#1
Benoît Chantemesse, Laetitia Betelli, Sébastien Solanas, Fabienne Vienney, Loïc Bollache, Alain Hartmann, Murielle Rochelet
A sensitive and inexpensive amperometric assay based on the electrochemical detection of the β-lactamase activity using the nitrocefin as substrate was developed for the rapid and quantitative detection of extended spectrum beta-lactamase-producing Escherichia coli (ESBL-EC) in urban wastewaters. The specific detection of ESBL-EC was achieved by culturing the filtered sample in a medium containing the cefotaxime supplemented or not with the potassium clavulanate inhibitor. This step was followed by the incubation of each subculture filtrate with the nitrocefin substrate which hydrolysis was monitored by amperometry using disposable carbon screen-printed sensors...
February 1, 2017: Water Research
https://www.readbyqxmd.com/read/27943428/synthesis-of-2-mercaptoacetyl-l-2-14-c-tryptophan-as-a-selective-metallo-%C3%AE-lactamase-inhibitor-via-2-14-c-indole-based-on-chiral-pool-strategy
#2
Gholamhossein Shirvani, Abbas Shockravi, Mohsen Amini, Nader Saemian
Metallo-beta-lactamase enzymes make bacteria resistant to a broad range of commonly used beta-lactam antibiotics. Several thiol derivatives of L-amino acids have been shown their inhibitory effects against the metallo-β-lactamase IMP-1. In this study, (2-mercaptoacetyl)-L-tryptophan as a new inhibitor of MBLs labeled with carbon-14 in the 2-position of the indole ring was prepared from [2-(14) C]indole as a key synthetic intermediate based on chiral pool strategy. The overall synthesis was carried out in ten-step with the overall radiochemical yield 3...
December 12, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27943223/in-vitro-activity-of-ceftolozane-tazobactam-alone-or-with-an-aminoglycoside-against-multi-drug-resistant-pseudomonas-aeruginosa-from-pediatric-cystic-fibrosis-patients
#3
Aimee M Dassner, Christina Sutherland, Jennifer Girotto, David P Nicolau
INTRODUCTION: Gram-negative multi-drug resistance is an emerging threat among pediatric patients with cystic fibrosis (CF). Ceftolozane/tazobactam (C/T) is an extended-spectrum cephalosporin/beta-lactamase inhibitor combination that has been shown to maintain activity against MDR P. aeruginosa isolates. The understanding of C/T effectiveness in pediatric patients is extremely limited. Minimum inhibitory concentration (MIC) testing and time-kill analyses were performed to better understand the antimicrobial susceptibility and potential role of C/T...
December 9, 2016: Infectious Diseases and Therapy
https://www.readbyqxmd.com/read/27891373/retrospective-comparison-of-clinical-characteristics-and-in-hospital-outcomes-among-diabetic-and-non-diabetic-adults-with-acute-pyelonephritis
#4
Shailesh C Trivedi, Sanjeev R Phatak, Renu S Trivedi
INTRODUCTION: Acute Pyelonephritis (APN) is a common infection in community. Diabetes Mellitus (DM) may have different effect on clinical characteristics and outcomes of APN compared to non-diabetic individuals. AIM: To compare clinical characteristics and assess outcomes of APN patients with and without DM. MATERIALS AND METHODS: A retrospective analysis of 122 patients with DM (n=61) and without DM (n=61) was conducted at a single, private, urban set-up from Gujarat, India...
October 2016: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/27890724/clinical-characteristics-and-antimicrobial-susceptibilities-of-anaerobic-bacteremia-in-an-acute-care-hospital
#5
Thean Yen Tan, Lily Siew Yong Ng, Lee Ling Kwang, Suma Rao, Li Ching Eng
This study investigated the clinical features of anaerobic bacteraemia in an acute-care hospital, and evaluated the antimicrobial susceptibility of these isolates to commonly available antibiotics. Microbiological and epidemiological data from 2009 to 2011were extracted from the laboratory information system and electronic medical records. One hundred and eleven unique patient episodes consisting of 116 anaerobic isolates were selected for clinical review and antibiotic susceptibility testing. Susceptibilities to amoxicillin-clavulanate, clindamycin, imipenem, metronidazole, moxifloxacin, penicillin and piperacillin-tazobactam were performed using Etest strips with categorical interpretations according to current CLSI breakpoints...
November 25, 2016: Anaerobe
https://www.readbyqxmd.com/read/27872080/classical-%C3%AE-lactamase-inhibitors-potentiate-the-activity-of-daptomycin-against-methicillin-resistant-staphylococcus-aureus-and-colistin-against-acinetobacter-baumannii
#6
George Sakoulas, Warren Rose, Andrew Berti, Joshua Olson, Jason Mungia, Poochit Nonejuie, Eleanna Sakoulas, Michael J Rybak, Joseph Pogliano, Victor Nizet
We asked whether beta-lactamase inhibitors (BLIs) increased the activity of daptomycin (DAP) against methicillin-resistant Staphylococcus aureus (MRSA), peptide antibiotic colistin (COL) against emerging Gram-negative nosocomial pathogen Acinetobacter baumannii, and human host defense peptide cathelicidin LL37 against either pathogen. DAP and LL37 kill curves were performed with or without BLIs against MRSA, vancomycin-intermediate S. aureus (VISA) and heterogeneous-VISA (hVISA). COL and LL37 kill curves were performed against A...
November 21, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27867083/trends-in-antimicrobial-resistance-among-bacteroides-species-and-parabacteroides-species-in-the-united-states-from-2010-2012-with-comparison-to-2008-2009
#7
REVIEW
D R Snydman, N V Jacobus, L A McDermott, E J C Goldstein, L Harrell, S G Jenkins, D Newton, R Patel, D W Hecht
The susceptibility trends for Bacteroides fragilis and related species against various antibiotics were determined using data from 3 years of surveillance (2010-2012) on 779 isolates referred by 7 medical centers. The antibiotic test panel included imipenem, ertapenem, meropenem, ampicillin-sulbactam, piperacillin-tazobactam, cefoxitin, clindamycin, moxifloxacin, tigecycline, linezolid, chloramphenicol and . MICs were determined using the agar dilution CLSI reference method. Carbapenem resistance remained low (range 1...
November 17, 2016: Anaerobe
https://www.readbyqxmd.com/read/27821441/%C3%AE-lactamase-inhibitors-enhance-the-synergy-between-%C3%AE-lactam-antibiotics-and-daptomycin-against-methicillin-resistant-staphylococcus-aureus
#8
Karl Evans R Henson, Juwon Yim, Jordan R Smith, George Sakoulas, Michael J Rybak
The evidence for using combination therapy for the treatment of serious methicillin-resistant Staphylococcus aureus (MRSA) infections is growing. In this study, we investigated the synergistic effect of daptomycin (DAP) combined with piperacillin-tazobactam and ampicillin-sulbactam against MRSA in time-kill experiments. Six of eight strains demonstrated synergy between DAP and the β-lactam-β-lactamase inhibitor (BLI) combination. In 5/8 strains, the synergy occurred only in the presence of the BLI, highlighting a role for BLIs in peptide-β-lactam synergy...
January 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27797327/-investigation-the-role-of-mutations-m182t-and-q39k-in-structure-of-beta-lactamase-tem-72-by-molecular-dynamics-method
#9
D S Shcherbinin, M Yu Rubtsova, V G Grigorenko, I V Uporov, A V Veselovsky, A M Egorov
Synthesis of b-lactamases is one of the common mechanisms of bacterial resistance to b-lactam antibiotics including penicillins and cephalosporins. The widespread use of antibiotics results in appearance of numerous extended-spectrum b-lactamase variants or resistance to inhibitors. Mutations of 92 residues of TEM type were found. Several mutations are the key mutations that determine the extension of spectrum of substrates. However, roles of the most associated mutations, located far from active site, remain unknown...
July 2016: Biomedit︠s︡inskai︠a︡ Khimii︠a︡
https://www.readbyqxmd.com/read/27766023/lower-body-mass-index-is-a-risk-factor-for-in-hospital-mortality-of-elderly-japanese-patients-treated-with-ampicillin-sulbactam
#10
Makoto Miura, Akiko Kuwahara, Akinori Tomozawa, Naoki Omae, Motohiro Yamamori, Kaori Kadoyama, Toshiyuki Sakaeda
Objectives: A retrospective examination was conducted to identify risk factors for in-hospital mortality of elderly patients (65 years or older) treated with the beta-lactam/beta-lactamase inhibitor combination antibiotic, ampicillin/sulbactam (ABPC/SBT). Methods: Clinical data from 96 patients who were hospitalized with infectious diseases and treated with ABPC/SBT (9 g/day or 12 g/day) were analyzed. Risk factors examined included demographic and clinical laboratory parameters. Parameter values prior to treatment and changes after treatment were compared between survivors and non-survivors...
2016: International Journal of Medical Sciences
https://www.readbyqxmd.com/read/27709861/risk-factor-analysis-of-ciprofloxacin-resistant-and-extended-spectrum-beta-lactamases-pathogen-induced-acute-bacterial-prostatitis-in-korea
#11
Young Lee, Dong Gi Lee, Sang Hyub Lee, Koo Han Yoo
The objectives of this study were to investigate risk factors and the incidence of ciprofloxacin resistance and extended-spectrum beta-lactamases (ESBL) in patients with acute bacterial prostatitis (ABP). We reviewed the medical records of 307 patients who were diagnosed with ABP between January 2006 and December 2015. The etiologic pathogens and risk factors for ciprofloxacin-resistant E. coli and ESBL-producing microbes, susceptibility to ciprofloxacin, and the incidence of ESBL in patients with ABP were described...
November 2016: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27610300/antibiotic-susceptibility-pattern-and-analysis-of-plasmid-profiles-of-pseudomonas-aeruginosa-from-human-animal-and-plant-sources
#12
Bamidele Tolulope Odumosu, Olabayo Ajetunmobi, Hannah Dada-Adegbola, Idowu Odutayo
Multidrug resistant organisms (MDROs) constitute a major public health threat globally. Clinical isolates of Pseudomonas aeruginosa remains one of the most studied MDROs however there is paucity of information regarding the susceptibility of its animal and plants isolates to antipseudomonas drug in Nigeria. From a total of 252 samples consisting of plants, animals and clinical samples, 54, 24 and 22 P. aeruginosa were isolated from vegetables, animals and clinical sources respectively. All the isolates were identified by standard biochemical methods...
2016: SpringerPlus
https://www.readbyqxmd.com/read/27572250/involvement-of-the-multidrug-efflux-pumps-in-betalactams-resistant-pseudomonas-aerugionsa-clinical-isolates-collected-from-burn-patients-in-iran
#13
Aslan Bijari, Leila Azimi, Fatemeh Fallah, Abdollah Ardebili, Elnaz Rastegar Lari, Abdolaziz Rastegar Lari
BACKGROUND: Multi-drug resistant P. aeruginosa has been increasing worldwide. Various mechanisms create this cross resistance in this bacterium including, acquisition beta-lactamases and intrinsic mechanisms, such as the presence of multidrug efflux pumps. Generally, multidrug efflux pumps inhibitor is used as a phenotypic method for the detection of active efflux pump systems. METHODS: In this study, 100 P. aeruginosa were collected from burn patients. Cefepime and imipenem resistant strains were isolated by disc diffusion agar and MIC...
2016: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/27528799/ceftazidime-avibactam-a-novel-cephalosporin-nonbeta-lactam-beta-lactamase-inhibitor-for-the-treatment-of-complicated-urinary-tract-infections-and-complicated-intra-abdominal-infections
#14
REVIEW
Jose A Hidalgo, Celeste M Vinluan, Nishaal Antony
There has been greater interest in developing additional antimicrobial agents due to the increasing health care costs and resistance resulting from bacterial pathogens to currently available treatment options. Gram-negative organisms including Enterobacteriaceae and Pseudomonas aeruginosa are some of the most concerning threats due to their resistance mechanisms: extended-spectrum beta-lactamase production and Klebsiella pneumoniae carbapenemase enzymes. Ceftazidime is a third-generation broad-spectrum cephalosporin with activity against P...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27527080/phase-1-study-of-the-safety-tolerability-and-pharmacokinetics-of-the-%C3%AE-lactamase-inhibitor-vaborbactam-rpx7009-in-healthy-adult-subjects
#15
David C Griffith, Jeffery S Loutit, Elizabeth E Morgan, Stephanie Durso, Michael N Dudley
Vaborbactam (formerly RPX7009) is a member of a new class of β-lactamase inhibitor with pharmacokinetic properties similar to those of many β-lactams, including carbapenems. The pharmacokinetics and safety of vaborbactam were evaluated in 80 healthy adult subjects in a first-in-human randomized, placebo-controlled, double-blind, sequential single- and multiple-ascending-dose study. A total of 10 dose cohorts were enrolled in the study, with 6 subjects randomized to receive 250 to 2,000 mg of vaborbactam and 2 subjects randomized to receive placebo in each cohort...
October 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27458232/crystal-structure-of-the-metallo-%C3%AE-lactamase-gob-in-the-periplasmic-dizinc-form-reveals-an-unusual-metal-site
#16
Jorgelina Morán-Barrio, María-Natalia Lisa, Nicole Larrieux, Salvador I Drusin, Alejandro M Viale, Diego M Moreno, Alejandro Buschiazzo, Alejandro J Vila
Metallo-beta-lactamases (MBLs) are broad-spectrum, Zn(II)-dependent lactamases able to confer resistance to virtually every β-lactam antibiotic currently available. The large diversity of active-site structures and metal content among MBLs from different sources has limited the design of a pan-MBL inhibitor. GOB-18 is a divergent MBL from subclass B3 that is expressed by the opportunistic Gram-negative pathogen Elizabethkingia meningoseptica This MBL is atypical, since several residues conserved in B3 enzymes (such as a metal ligand His) are substituted in GOB enzymes...
October 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27414088/kinetics-of-antimicrobial-activity-of-amoxicillin-clavulanic-acid-and-metronidazole-against-%C3%AE-lactamase-producing-bacteroides-fragilis-group
#17
J A García-Rodríguez, J E García Sánchez, I Trujillano, J L Muñoz-Bellido
Bacteroides fragilis group are the most common anaerobic bacteria isolated in clinical specimens. The use of a beta-lactam with a β-lactamase inhibitor should result in a marked increase in the group's sensitivity to the β-lactams. Since the activity (MIC) shown by the amoxicillin + clavulanic acid combination against Bacteroides fragilis group is good, other parameters of in vitro activity have been studied. This study was also done with metronidazole. The minimum inhibitory concentration (MIC) was determined in 26 strains of Bacteroides fragilis group (14 B...
February 1990: Journal of Chemotherapy
https://www.readbyqxmd.com/read/27353461/an-evolutionarily-conserved-allosteric-site-modulates-beta-lactamase-activity
#18
Fatma Gizem Avci, Fatma Ece Altinisik, Didem Vardar Ulu, Elif Ozkirimli Olmez, Berna Sariyar Akbulut
Declining efficiency of antibiotic-inhibitor combinatorial therapies in treating beta-lactamase mediated resistance necessitates novel inhibitor development. Allosteric inhibition offers an alternative to conventional drugs that target the conserved active site. Here, we show that the evolutionarily conserved PWP triad located at the N-terminus of the H10 helix directly interacts with the allosteric site in TEM-1 beta-lactamase and regulates its activity. While point mutations in the PWP triad preserve the overall secondary structures around the allosteric site, they result in a more open and dynamic global structure with decreased chemical stability and increased aggregation propensity...
2016: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/27297743/analysis-of-the-2015-american-and-european-guidelines-for-the-management-of-infective-endocarditis
#19
REVIEW
P Tattevin, J-L Mainardi
The optimal management of infective endocarditis requires a broad range of expertise (infectious disease specialists, cardiologists, microbiologists, cardiac surgeons, and intensivists). Given the low level of evidence currently available to support the management of infective endocarditis, international guidelines have always been particularly awaited and rather well implemented. Their cautious analysis of the medical literature and the range of expertise combined within the groups in charge of these guidelines are usually broadly acknowledged and respected...
December 2016: Médecine et Maladies Infectieuses
https://www.readbyqxmd.com/read/27238248/antibiotic-consumption-in-turkish-hospitals-a-multi-centre-point-prevalence-study
#20
Ertugrul Guclu, Aziz Ogutlu, Oguz Karabay, Tuna Demirdal, Ibrahim Erayman, Salih Hosoglu, Vedat Turhan, Serpil Erol, Nefise Oztoprak, Ayse Batirel, Fatma Aybala Altay, Gulsum Kaya, Mustafa Karahocagil, Hamdi Sozen, Mustafa Yildirim, Funda Kocak, Bahri Teker
This multi-centre study aimed to determine the antibiotic consumption in Turkish hospitals by point prevalence. Antibiotic consumption of 14 centres was determined using the DDD method. Among hospitalized patients, 44.8% were using antibiotics and the total antibiotic consumption was 674.5 DDD/1000 patient-days (DPD). 189.6 (28%) DPD of the antibiotic consumption was restricted while 484.9 (72%) DPD was unrestricted. Carbapenems (24%) and beta lactam/beta lactamase inhibitors (ampicillin-sulbactam or amoxicillin-clavulanate; 22%) were the most commonly used restricted and unrestricted antibiotics...
May 30, 2016: Journal of Chemotherapy
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