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beta-lactamase inhibitor

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https://www.readbyqxmd.com/read/28822333/virtual-screening-and-repositioning-of-inconclusive-molecules-of-beta-lactamase-bioassays-a-data-mining-approach
#1
Akshata Gad, Andrew Titus Manuel, Jinuraj K R, Lijo John, Sajeev R, Shanmuga Priya V G, Abdul Jaleel U C
This study focuses on the best possible way forward in utilizing inconclusive molecules of PubChem bioassays AID 1332, AID 434987 and AID 434955, which are related to beta-lactamase inhibitors of Mycobacterium tuberculosis (Mtb). The inadequacy in the experimental methods that were observed during the invitro screening resulted in an inconclusive dataset. This could be due to certain moieties present within the molecules. In order to reconsider such molecules, insilico methods can be suggested in place of invitro methods For instance, datamining and medicinal chemistry methods: have been adopted to prioritise the inconclusive dataset into active or inactive molecules...
July 29, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28799307/guiding-principles-for-the-use-of-fluroquinolones-in-out-patient-community-settings-of-india-panel-consensus
#2
Agam Vora, K Krishnaprasad
INTRODUCTION: Respiratory tract infections have been an important cause of morbidity and mortality worldwide that is looming large especially in context of antibiotic resistance that is confronted both by a pulmonologist as well as a general practitioner. A reflection to this trend has been the rising phenomenon of MICs as shown the respiratory pathogens towards conventional antibiotics including macrolides or β lactam/β lactamase inhibitor combinations. Respiratory fluoroquinolones offer broad yet potent cover of respiratory pathogens leading to their obvious choice for empirical therapy for clinical persisters or high risk cases with prior history of antibiotics not-withstanding the clinical concerns in tropical countries...
August 2017: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/28697720/early-onset-pneumonia-after-liver-transplant-microbial-causes-risk-factors-and-outcomes-mansoura-university-egypt-experience
#3
Mohammad Khairy El-Badrawy, Raed El-Metwaly Ali, Amr Yassen, Mohammad Ahmad AbouElela, Rehab Ahmad Elmorsey
OBJECTIVES: Pneumonia has a negative effect on the outcome of liver transplant. Our aim was to analyze early-onset pneumonia that developed within the first month after transplant. MATERIALS AND METHODS: This prospective single-center study included 56 adult living-donor liver transplant recipients; those who developed early-onset pneumonia based on clinical and radiologic criteria were investigated as to causative pathogens and then followed up and compared with other recipients without pneumonia to illustrate risk factors, outcomes, and related mortality of posttransplant pneumonia...
July 11, 2017: Experimental and Clinical Transplantation
https://www.readbyqxmd.com/read/28634829/potential-inhibitory-effect-of-indolizine-derivatives-on-the-two-enzymes-nicotinamide-phosphoribosyltransferase-and-beta-lactamase-a-molecular-dynamics-study
#4
Beata Szefler, Przemysław Czeleń
Nicotinamide phosphoribosyl-transferases (NAMPT) are enzymes that play a role in targeting cancer metabolism, while beta lactamases are involved in bacterial resistance to beta-lactam antibiotics. Many protein inhibitors exhibit such property which is often correlated with their cellular potency. In order to understand such a phenomenon, the present article conducts an analysis of the dynamic behavior of complexes formed by the inhibitors, that is indolizine derivatives, with the studied enzymes. Both docking and molecular dynamics led to identification of their interactions and showed the mechanism of inhibition of the two studied enzymes...
July 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28631121/-prudent-use-of-antimicrobial-prophylaxis-prevention-of-increasing-antibiotic-resistance
#5
REVIEW
C Hein, A Pilatz, F M E Wagenlehner
BACKGROUND: The use of peri-operative antimicrobial prophylaxis during urological procedures to prevent postoperative complications is very common. OBJECTIVES: What kind of recommendations for reasonable use of peri-operative antimicrobial prophylaxis during urological procedures to prevent increasing antibiotic resistance and postoperative complications exist? METHODS: Review of evidence-based recommendations from literature and current Guidelines of the EAU...
June 19, 2017: Der Urologe. Ausg. A
https://www.readbyqxmd.com/read/28574718/calibration-of-1-2-4-triazole-3-thione-an-original-zn-binding-group-of-metallo-%C3%AE-lactamase-inhibitors-validation-of-a-polarizable-mm-md-potential-by-quantum-chemistry
#6
Karolina Kwapien, Mirna Damergi, Serge Nader, Léa El Khoury, Zeina Hobaika, Richard G Maroun, Jean-Philip Piquemal, Laurent Gavara, Dorothée Berthomieu, Jean-François Hernandez, Nohad Gresh
In the context of the SIBFA polarizable molecular mechanics/dynamics (PMM/PMD) procedure, we report the calibration and a series of validation tests for the 1,2,4-triazole-3-thione (TZT) heterocycle. TZT acts as the chelating group of inhibitors of dizinc metallo-β-lactamases (MBL), an emerging class of Zn-dependent bacterial enzymes, which by cleaving the β-lactam bond of most β-lactam antibiotics are responsible for the acquired resistance of bacteria to these drugs. Such a study is indispensable prior to performing PMD simulations of complexes of TZT-based inhibitors with MBL's, on account of the anchoring role of TZT in the dizinc MBL recognition site...
June 22, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28483952/multicenter-study-of-outcomes-with-ceftazidime-avibactam-in-patients-with-carbapenem-resistant-enterobacteriaceae-infections
#7
Madeline King, Emily Heil, Safia Kuriakose, Tiffany Bias, Vanthida Huang, Claudine El-Beyrouty, Dorothy McCoy, Jon Hiles, Lynette Richards, Julianne Gardner, Nicole Harrington, Kenneth Biason, Jason C Gallagher
Ceftazidime-avibactam is a novel cephalosporin-beta-lactamase inhibitor combination that is active against many carbapenem-resistant Enterobacteriaceae (CRE). We describe a retrospective chart review for 60 patients who received ceftazidime-avibactam for a CRE infection. In-hospital mortality was 32%, 53% of patients had microbiological cure, and 65% had clinical success. In this severely ill population with CRE infections, ceftazidime-avibactam was an appropriate option.
July 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28465626/synthesis-and-biological-evaluation-of-indole-core-based-derivatives-with-potent-antibacterial-activity-against-resistant-bacterial-pathogens
#8
Wei Hong, Jingyang Li, Zhe Chang, Xiaoli Tan, Hao Yang, Yifan Ouyang, Yanhui Yang, Sargit Kaur, Ian C Paterson, Yun Fong Ngeow, Hao Wang
The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management. To exacerbate this problem, there is currently a serious lack of antibacterial agents that are designed to target extremely drug-resistant bacterial strains. Here we describe the design, synthesis and antibacterial testing of a series of 40 novel indole core derivatives, which are predicated by molecular modeling to be potential glycosyltransferase inhibitors. Twenty of these derivatives were found to show in vitro inhibition of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus...
July 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28377310/risk-factors-for-extended-spectrum-%C3%AE-lactamase-producing-escherichia-coli-urinary-tract-infection-in-the-community-in-denmark-a-case-control-study
#9
M Søgaard, U Heide-Jørgensen, J P Vandenbroucke, H C Schønheyder, C M J E Vandenbroucke-Grauls
OBJECTIVE: To verify the role of proton pump inhibitors (PPI) and nitrofurantoin, which have appeared as novel risk factors for carriage of extended-spectrum β-lactamase (ESBL) -producing Escherichia coli, as risk factors for ESBL E. coli urinary tract infection (UTI). We included known risk factors to ascertain whether our findings are comparable with those of previous studies. METHODS: Population-based case-control study including 339 cases with community-onset ESBL E...
April 1, 2017: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/28367020/comparison-of-four-phenotypic-methods-for-detection-of-metallo-%C3%AE-lactamase-producing-gram-negative-bacteria-in-rural-teaching-hospital
#10
Chinjal A Panchal, Sweta Sunil Oza, Sanjay J Mehta
CONTEXT: Metallo-β-lactamase (MBL)-producing bacteria lead to resistance to carbapenem an antibiotic that used as the last resort for treatment of multidrug-resistant bacteria, extended spectrum beta-lactamases, and AmpC β-lactamase-producing Gram-negative bacteria (GNB). The emergence of MBL-producing GNB is challenge to microbiology laboratories because there are no standardized guidelines available to detect them. The aim of this study was to compare four phenotypic methods to detect MBL production in GNB and to determine antibiotic sensitivity of MBL-producing isolates...
April 2017: Journal of Laboratory Physicians
https://www.readbyqxmd.com/read/28343258/variation-of-antibiotic-consumption-and-its-correlated-factors-in-turkey
#11
Ayfer Sahin, Ahmet Akici, Volkan Aydin, Bahar Melik, Mesil Aksoy, Ali Alkan
BACKGROUND: Presentation of antibiotic utilization data by reliable and comparable analyses constitutes an important way of ensuring rational use of antibiotics. This study aimed to evaluate antibiotic consumption (AC) of Turkey by each city/region and to investigate any association of such consumption with socio-economic factors. METHOD: For 81 provinces and 12 regions in Turkey, AC data from IMS (Intercontinental Medical Statistics) in 2011 was analyzed in accordance with "ATC/DDD, DID" (Anatomical Therapeutic Chemical/Defined Daily Doses, DID = DDD/1000 inhabitants/day) methodology supported by World Health Organization...
March 25, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28338347/ceftazidime-avibactam-novel-antimicrobial-combination-for-the-treatment-of-complicated-urinary-tract-infections
#12
Jakhongir F Alidjanov, Moritz Fritzenwanker, Ivan Hoffman, Florian M Wagenlehner
Ceftazidime-avibactam is a combination of a third-generation cephalosporin and a novel non-beta-lactam beta-lactamase inhibitor. This combination was recently recommended for the treatment of complicated urinary tract infections, including acute pyelonephritis, in adults with limited or no alternative treatment options. The current review is aimed to determine activity, efficacy and safety of ceftazidime-avibactam in the treatment of patients with complicated urinary tract infections.
March 24, 2017: Future Microbiology
https://www.readbyqxmd.com/read/28303449/novel-beta-lactamase-inhibitors-unlocking-their-potential-in-therapy
#13
REVIEW
Darren Wong, David van Duin
Carbapenem-resistant Enterobacteriaceae are amongst the most feared pathogens due to severely limited treatment options. In response to this threat, three novel β-lactamase inhibitors have been developed in an attempt to reinvigorate and sustain our current antimicrobial therapies. Avibactam, vaborbactam, and relebactam are inhibitor agents with high affinity to Ambler class A and C β-lactamases and favorable outcomes in current clinical trials. However, although they do possess key similarities, these agents have unique differences which may have important clinical implications...
April 2017: Drugs
https://www.readbyqxmd.com/read/28299853/the-effect-of-a-beta-lactamase-inhibitor-peptide-on-bacterial-membrane-structure-and-integrity-a-comparative-study
#14
COMPARATIVE STUDY
Begum Alaybeyoglu, Bilge Gedik Uluocak, Berna Sariyar Akbulut, Elif Ozkirimli
Co-administration of beta-lactam antibiotics and beta-lactamase inhibitors has been a favored treatment strategy against beta-lactamase-mediated bacterial antibiotic resistance, but the emergence of beta-lactamases resistant to current inhibitors necessitates the discovery of novel non-beta-lactam inhibitors. Peptides derived from the Ala46-Tyr51 region of the beta-lactamase inhibitor protein are considered as potent inhibitors of beta-lactamase; unfortunately, peptide delivery into the cell limits their potential...
May 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28289035/wck-5107-zidebactam-and-wck-5153-are-novel-inhibitors-of-pbp2-showing-potent-%C3%AE-lactam-enhancer-activity-against-pseudomonas-aeruginosa-including-multidrug-resistant-metallo-%C3%AE-lactamase-producing-high-risk-clones
#15
Bartolome Moya, Isabel M Barcelo, Sachin Bhagwat, Mahesh Patel, German Bou, Krisztina M Papp-Wallace, Robert A Bonomo, Antonio Oliver
Zidebactam and WCK 5153 are novel β-lactam enhancers that are bicyclo-acyl hydrazides (BCH), derivatives of the diazabicyclooctane (DBO) scaffold, targeted for the treatment of serious infections caused by highly drug-resistant Gram-negative pathogens. In this study, we determined the penicillin-binding protein (PBP) inhibition profiles and the antimicrobial activities of zidebactam and WCK 5153 against Pseudomonas aeruginosa, including multidrug-resistant (MDR) metallo-β-lactamase (MBL)-producing high-risk clones...
June 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28247443/acute-kidney-injury-in-patients-treated-with-iv-beta-lactam-beta-lactamase-inhibitor-combinations
#16
W Cliff Rutter, David S Burgess
STUDY OBJECTIVE: Increased acute kidney injury (AKI) incidence has been reported in patients receiving piperacillin-tazobactam (PTZ) therapy compared with other β-lactams. The authors sought to determine if the addition of β-lactamase inhibitors impacts AKI incidence by comparing patients treated with PTZ or ampicillin-sulbactam (SAM). DESIGN: Retrospective cohort study. SETTING: Large academic tertiary care hospital. PATIENTS: Overall, 2448 patients received PTZ (n=1836) or SAM (n=612) for at least 48 hours between September 1, 2007, and September 30, 2015...
May 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28244482/the-microbial-etiology-and-antimicrobial-susceptibility-of-bloodstream-infections-in-patients-with-cancer-at-a-private-tertiary-care-hospital-in-mumbai-india
#17
T Singhal, S Shah, R Naik
BACKGROUND: Knowledge of the etiology and antimicrobial susceptibility of blood stream infections in patients with cancer is crucial to design empirical therapy regimes. METHODS: This is a prospective observational study at a tertiary care private hospital in Mumbai, India from Nov 2009 - Dec 2014. RESULTS: A total of 62 episodes of blood stream infections in 57 patients with cancer were recorded during the study period. Analysis was limited to 52 isolates from 49 episodes in 45 patients...
July 2016: Indian Journal of Cancer
https://www.readbyqxmd.com/read/28193660/antimicrobial-resistance-of-escherichia-coli-urinary-isolates-in-the-veterans-affairs-health-care-system
#18
Haley J Morrill, Jacob B Morton, Aisling R Caffrey, Lan Jiang, David Dosa, Leonard A Mermel, Kerry L LaPlante
We reviewed data for almost 300,000 clinical Escherichia coli urinary isolates (collected in 2009 through 2013) from 127 inpatient and outpatient facilities, to assess antibiotic resistance among Veterans Affairs health care system patients using Clinical and Laboratory Standards Institute and Centers for Disease Control and Prevention National Healthcare Safety Network definitions or guidance. Rates of resistance to amoxicillin or ampicillin/β-lactamase inhibitors were approximately 40% and rates of resistance to fluoroquinolones and trimethoprim-sulfamethoxazole approached 30%...
May 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28164610/an-investigation-of-the-frequency-of-upper-respiratory-tract-infection-pathogens-and-their-antibiotic-patterns-in-tonsils-and-adenoids-of-adenotonsillectomy-patients
#19
Yasar Nakipoglu, Gulsen Gunel, Deniz Kanliada, Levent Aydemir, Nezahat Gurler, Bulent Gurler
BACKGROUND: We aimed to investigate the potentially pathogenic bacteria of upper respiratory tract infections (URTIs) and their susceptibilities to different antibiotics. METHODS: Two-hundred adenoid and tonsil specimens from 100 patients who had undergone adenotonsillectomy were obtained and analyzed bacteriologically. Identification of the pathogens was made by conventional or commercial identification systems and antibiotic susceptibility tests were carried out by disk diffusion method...
August 1, 2016: Clinical Laboratory
https://www.readbyqxmd.com/read/28157141/icu-acquisition-rate-risk-factors-and-clinical-significance-of-digestive-tract-colonization-with-extended-spectrum-beta-lactamase-producing-enterobacteriaceae-a-systematic-review-and-meta-analysis
#20
REVIEW
Marios Detsis, Styliani Karanika, Eleftherios Mylonakis
OBJECTIVE: To evaluate the acquisition rate, identify risk factors, and estimate the risk for subsequent infection, associated with the colonization of the digestive tract with extended-spectrum beta-lactamase-producing Enterobacteriaceae during ICU-hospitalization. DATA SOURCES: PubMed, EMBASE, and reference lists of all eligible articles. STUDY SELECTION: Included studies provided data on ICU-acquired colonization with extended-spectrum beta-lactamase-producing Enterobacteriaceae in previously noncolonized and noninfected patients and used the double disk synergy test for extended-spectrum beta-lactamase-producing Enterobacteriaceae phenotypic confirmation...
April 2017: Critical Care Medicine
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