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https://www.readbyqxmd.com/read/28902135/point-prevalence-surveys-of-antimicrobial-use-among-hospitalized-children-in-six-hospitals-in-india-in-2016
#1
Sumanth Gandra, Sanjeev K Singh, Dasaratha R Jinka, Ravishankar Kanithi, Ashok K Chikkappa, Anita Sharma, Dhanya Dharmapalan, Anil Kumar Vasudevan, Onkaraiah Tunga, Akhila Akula, Garima Garg, Yingfen Hsia, Srinivas Murki, Gerardo Alvarez-Uria, Mike Sharland, Ramanan Laxminarayan
The prevalence of antimicrobial resistance in India is among the highest in the world. Antimicrobial use in inpatient settings is an important driver of resistance, but is poorly characterized, particularly in hospitalized children. In this study, conducted as part of the Global Antimicrobial Resistance, Prescribing, and Efficacy in Neonates and Children (GARPEC) project, we examined the prevalence of and indications of antimicrobial use, as well as antimicrobial agents used among hospitalized children by conducting four point prevalence surveys in six hospitals between February 2016 and February 2017...
September 13, 2017: Antibiotics
https://www.readbyqxmd.com/read/28892020/identification-of-staphylococcus-aureus-cellular-pathways-affected-by-the-stilbenoid-lead-drug-sk-03-92-using-a-microarray
#2
William R Schwan, Rebecca Polanowski, Paul M Dunman, Sara Medina-Bielski, Michelle Lane, Marc Rott, Lauren Lipker, Amy Wescott, Aaron Monte, James M Cook, Douglas D Baumann, V V N Phani Babu Tiruveedhula, Christopher M Witzigmann, Cassandra Mikel, Md Toufiqur Rahman
The mechanism of action for a new lead stilbene compound coded SK-03-92 with bactericidal activity against methicillin-resistant Staphylococcus aureus (MRSA) is unknown. To gain insight into the killing process, transcriptional profiling was performed on SK-03-92 treated vs. untreated S. aureus. Fourteen genes were upregulated and 38 genes downregulated by SK-03-92 treatment. Genes involved in sortase A production, protein metabolism, and transcriptional regulation were upregulated, whereas genes encoding transporters, purine synthesis proteins, and a putative two-component system (SACOL2360 (MW2284) and SACOL2361 (MW2285)) were downregulated by SK-03-92 treatment...
September 11, 2017: Antibiotics
https://www.readbyqxmd.com/read/28892001/synthesis-and-immunological-evaluation-of-virus-like-particle-milbemycin-a%C3%A2-a%C3%A2-conjugates
#3
Andris Zeltins, Māris Turks, Dace Skrastina, Jevgeņija Lugiņina, Ieva Kalnciema, Ina Balke, Ērika Bizdēna, Vitalijs Skrivelis
Milbemycins are macrolide antibiotics with a broad spectrum of nematocidal, insecticidal, and acaricidal activity. To obtain milbemycin A₃/A₄ derivatives suitable for chemical conjugation to protein carriers (milbemycin haptens), succinate linker and a novel 17-atom-long linker containing a terminal carboxylic acid group were attached to the milbemycin core in a protecting group-free synthesis. The obtained milbemycin A₃/A₄ derivatives were coupled to Potato virus Y-like nanoparticles by the activated ester method...
September 11, 2017: Antibiotics
https://www.readbyqxmd.com/read/28813003/self-assessment-of-antimicrobial-stewardship-in-primary-care-self-reported-practice-using-the-target-primary-care-self-assessment-tool
#4
Rebecca Owens, Leah Ffion Jones, Michael Moore, Dirk Pilat, Cliodna McNulty
Multifaceted antimicrobial stewardship (AMS) interventions including: antibiotic guidance, reviews of antibiotic use using audits, education, patient facing materials, and self-assessment, are successful in improving antimicrobial use. We aimed to measure the self-reported AMS activity of staff completing a self-assessment tool (SAT). The Royal College of General Practitioners (RCGP)/Public Health England (PHE) SAT enables participants considering an AMS eLearning course to answer 12 short questions about their AMS activities...
August 16, 2017: Antibiotics
https://www.readbyqxmd.com/read/28767074/comparative-study-on-antistaphylococcal-activity-of-lipopeptides-in-various-culture-media
#5
Maciej Jaśkiewicz, Damian Neubauer, Wojciech Kamysz
Staphylococcus aureus bacteria are one of the leading microorganisms responsible for nosocomial infections as well as being the primary causative pathogen of skin and wound infections. Currently, the therapy of staphylococcal diseases faces many difficulties, due to a variety of mechanisms of resistance and virulence factors. Moreover, a number of infections caused by S. aureus are connected with biofilm formation that impairs effectiveness of the therapy. Short cationic lipopeptides that are designed on the basis of the structure of antimicrobial peptides are likely to provide a promising alternative to conventional antibiotics...
August 2, 2017: Antibiotics
https://www.readbyqxmd.com/read/28677631/macromolecular-conjugate-and-biological-carrier-approaches-for-the-targeted-delivery-of-antibiotics
#6
REVIEW
Nhan Dai Thien Tram, Pui Lai Rachel Ee
For the past few decades, the rapid rise of antibiotic multidrug-resistance has presented a palpable threat to human health worldwide. Meanwhile, the number of novel antibiotics released to the market has been steadily declining. Therefore, it is imperative that we utilize innovative approaches for the development of antimicrobial therapies. This article will explore alternative strategies, namely drug conjugates and biological carriers for the targeted delivery of antibiotics, which are often eclipsed by their nanomedicine-based counterparts...
July 4, 2017: Antibiotics
https://www.readbyqxmd.com/read/28657596/antibacterial-activity-and-toxicity-of-analogs-of-scorpion-venom-isct-peptides
#7
Roberto de la Salud Bea, Adam F Petraglia, Michael R Ascuitto, Quentin M Buck
Seven analogs of the natural, α-helix peptides IsCT1 and IsCT2-found in the venom of scorpion Opithancatus Madagascariensis-have been synthesized and tested to compare their antibacterial and hemolytic activity against natural peptides. In general, results show that increasing hydrophobicity by substituting positions 5 and 9 of the sequences with alanine, valine, and leucine, enhances antibacterial activity. However, this also increases hemolytic activity. The analog with an increased net positive charge from +1 to +3 produces moderate bacterial growth inhibition but also has high hemolytic activity...
June 28, 2017: Antibiotics
https://www.readbyqxmd.com/read/28587316/bacteria-from-animals-as-a-pool-of-antimicrobial-resistance-genes
#8
REVIEW
Maria Angeles Argudín, Ariane Deplano, Alaeddine Meghraoui, Magali Dodémont, Amelie Heinrichs, Olivier Denis, Claire Nonhoff, Sandrine Roisin
Antimicrobial agents are used in both veterinary and human medicine. The intensive use of antimicrobials in animals may promote the fixation of antimicrobial resistance genes in bacteria, which may be zoonotic or capable to transfer these genes to human-adapted pathogens or to human gut microbiota via direct contact, food or the environment. This review summarizes the current knowledge of the use of antimicrobial agents in animal health and explores the role of bacteria from animals as a pool of antimicrobial resistance genes for human bacteria...
June 6, 2017: Antibiotics
https://www.readbyqxmd.com/read/28441360/erythromycin-modification-that-improves-its-acidic-stability-while-optimizing-it-for-local-drug-delivery
#9
Erika L Cyphert, Jaqueline D Wallat, Jonathan K Pokorski, Horst A von Recum
The antibiotic erythromycin has limited efficacy and bioavailability due to its instability and conversion under acidic conditions via an intramolecular dehydration reaction. To improve the stability of erythromycin, several analogs have been developed-such as azithromycin and clarithromycin-which decrease the rate of intramolecular dehydration. We set out to build upon this prior work by developing a conjugate of erythromycin with improved pH stability, bioavailability, and preferential release from a drug delivery system directly at the low pH of an infection site...
April 25, 2017: Antibiotics
https://www.readbyqxmd.com/read/28327498/activity-of-sulfa-drugs-and-their-combinations-against-stationary-phase-b-burgdorferi-in-vitro
#10
Jie Feng, Shuo Zhang, Wanliang Shi, Ying Zhang
Lyme disease is a most common vector-borne disease in the US. Although the majority of Lyme patients can be cured with the standard two- to four-week antibiotic treatment, at least 10%-20% of patients continue to suffer from prolonged post-treatment Lyme disease syndrome (PTLDS). While the cause for this is unclear, one possibility is that persisting organisms are not killed by current Lyme antibiotics. In our previous studies, we screened an FDA drug library and an NCI compound library on B. burgdorferi and found some drug hits including sulfa drugs as having good activity against B...
March 22, 2017: Antibiotics
https://www.readbyqxmd.com/read/28272350/a-risk-assessment-of-antibiotic-pan-drug-resistance-in-the-uk-bayesian-analysis-of-an-expert-elicitation-study
#11
Daniel Carter, André Charlett, Stefano Conti, Julie V Robotham, Alan P Johnson, David M Livermore, Tom Fowler, Mike Sharland, Susan Hopkins, Neil Woodford, Philip Burgess, Stephen Dobra
To inform the UK antimicrobial resistance strategy, a risk assessment was undertaken of the likelihood, over a five-year time-frame, of the emergence and widespread dissemination of pan-drug-resistant (PDR) Gram-negative bacteria that would pose a major public health threat by compromising effective healthcare delivery. Subsequent impact over five- and 20-year time-frames was assessed in terms of morbidity and mortality attributable to PDR Gram-negative bacteraemia. A Bayesian approach, combining available data with expert prior opinion, was used to determine the probability of the emergence, persistence and spread of PDR bacteria...
March 7, 2017: Antibiotics
https://www.readbyqxmd.com/read/28241458/bulgecin%C3%A2-a-%C3%A2-the%C3%A2-key%C3%A2-to%C3%A2-a%C3%A2-broad-spectrum%C3%A2-inhibitor%C3%A2-that%C3%A2-targets%C3%A2-lytic%C3%A2-transglycosylases
#12
Allison H Williams, Richard Wheeler, Constance Thiriau, Ahmed Haouz, Muhamed-Kheir Taha, Ivo G Boneca
Lytic transglycosylases (Lts) are involved in recycling, cell division, and metabolism of the peptidoglycan. They have been understudied for their usefulness as potential antibacterial targets due to their high redundancy in Gram-negative bacteria. Bulgecin A is an O-sulphonated glycopeptide that targets primarily soluble lytic tranglycosylases (Slt). It has been shown that bulgecin A increases the efficacy of β-lactams that target penicillin bindings proteins (PBPs). Here, we present the high-resolution crystal structure of LtgA from Neisseria meningitidis strain MC58, a membrane bound homolog of Escherichia coli Slt, in complex with bulgecin A...
February 22, 2017: Antibiotics
https://www.readbyqxmd.com/read/28208717/final-demonstration-of-the-co-identity-of-lipiarmycin-a3-and-tiacumicin-b-fidaxomicin-through-single-crystal-x-ray-analysis
#13
Stefano Serra, Luciana Malpezzi, Angelo Bedeschi, Claudio Fuganti, Piera Fonte
Lipiarmycin A3 and tiacumicin B possess the same chemical structure and have been considered identical till recently, when some authors have suggested the possibility of a minor difference between the chemical structures of the two antibiotics. In this work we performed a comparative X-ray analysis of lipiarmycin A3 and tiacumicin B. Although the commercial samples of the aforementioned compounds crystallize into two different crystal systems-evidently due to the different crystallization conditions-their chemical structures are identical...
February 8, 2017: Antibiotics
https://www.readbyqxmd.com/read/28178179/diminished-antimicrobial-peptide-and-antifungal-antibiotic-activities-against-candida-albicans-in-denture-adhesive
#14
Amber M Bates, Jorge L Garaicoa, Carol L Fischer, Kim A Brogden
The underlying causes of denture stomatitis may be related to the long-term use of adhesives, which may predispose individuals to oral candidiasis. In this study, we hypothesize that antimicrobial peptides and antifungal antibiotics have diminished anti-Candida activities in denture adhesive. To show this, nine antimicrobial peptides and five antifungal antibiotics with and without 1.0% denture adhesive were incubated with Candida albicans strains ATCC 64124 and HMV4C in radial diffusion assays. In gels with 1...
February 6, 2017: Antibiotics
https://www.readbyqxmd.com/read/28165431/moxifloxacin-increases-heart-rate-in-humans
#15
Jay W Mason, Thomas E Moon
(1) Background: We assessed the effect of moxifloxacin on heart rate, and reviewed the heart rate effects of other antibiotics; (2) Methods: A total of 335 normal volunteers had 12-lead electrocardiograms recorded at multiple time points before and during treatment with moxifloxacin and with placebo in seven consecutive, thorough QT studies of crossover design; (3) Results: The average baseline heart rate across the seven studies was 61.5 bpm. The heart rate after moxifloxacin dosing was analyzed at five time points shared by all seven studies (hours 1, 2, 3, 12 and 24)...
February 5, 2017: Antibiotics
https://www.readbyqxmd.com/read/28134858/docking-into-mycobacterium-tuberculosis-thioredoxin-reductase-protein-yields-pyrazolone-lead-molecules-for-methicillin-resistant-staphylococcus-aureus
#16
Noreena L Sweeney, Lauren Lipker, Alicia M Hanson, Chris J Bohl, Katie E Engel, Kelsey S Kalous, Mary E Stemper, Daniel S Sem, William R Schwan
The thioredoxin/thioredoxin reductase system (Trx/TrxR) is an attractive drug target because of its involvement in a number of important physiological processes, from DNA synthesis to regulating signal transduction. This study describes the finding of pyrazolone compounds that are active against Staphylococcus aureus. Initially, the project was focused on discovering small molecules that may have antibacterial properties targeting the Mycobacterium tuberculosis thioredoxin reductase. This led to the discovery of a pyrazolone scaffold-containing compound series that showed bactericidal capability against S...
January 28, 2017: Antibiotics
https://www.readbyqxmd.com/read/28098814/thioridazine-a-non-antibiotic-drug-highly-effective-in-combination-with-first-line-anti-tuberculosis-drugs-against-any-form-of-antibiotic-resistance-of-mycobacterium-tuberculosis-due-to-its-multi-mechanisms-of-action
#17
REVIEW
Leonard Amaral, Miguel Viveiros
This review presents the evidence that supports the use of thioridazine (TZ) for the therapy of a pulmonary tuberculosis infection regardless of its antibiotic resistance status. The evidence consists of in vitro and ex vivo assays that demonstrate the activity of TZ against all encountered Mycobacterium tuberculosis (Mtb) regardless of its antibiotic resistance phenotype, as well as in vivo as a therapy for mice infected with multi-drug resistant strains of Mtb, or for human subjects infected with extensively drug resistant (XDR) Mtb...
January 14, 2017: Antibiotics
https://www.readbyqxmd.com/read/28098784/fused-ring-oxazolopyrrolopyridopyrimidine-systems-with-gram-negative-activity
#18
Yiyuan Chen, Jonathan G Moloney, Kirsten E Christensen, Mark G Moloney
Fused polyheterocyclic derivatives are available by annulation of a tetramate scaffold, and been shown to have antibacterial activity against a Gram-negative, but not a Gram-positive, bacterial strain. While the activity is not potent, these systems are structurally novel showing, in particular, a high level of polarity, and offer potential for the optimization of antibacterial activity.
January 13, 2017: Antibiotics
https://www.readbyqxmd.com/read/27983678/quorum-sensing-and-the-use-of-quorum-quenchers-as-natural-biocides-to-inhibit-sulfate-reducing-bacteria
#19
Giantommaso Scarascia, Tiannyu Wang, Pei-Ying Hong
Sulfate-reducing bacteria (SRB) are one of the main protagonist groups of biocorrosion in the seawater environment. Given their principal role in biocorrosion, it remains a crucial task to develop strategies to reduce the abundance of SRBs. Conventional approaches include the use of biocides and antibiotics, which can impose health, safety, and environmental concerns. This review examines an alternative approach to this problem. This is achieved by reviewing the role of quorum sensing (QS) in SRB populations and its impact on the biofilm formation process...
December 15, 2016: Antibiotics
https://www.readbyqxmd.com/read/27983590/conformational-response-of-30s-bound-if3-to-a-site-binders-streptomycin-and-kanamycin
#20
Roberto Chulluncuy, Carlos Espiche, Jose Alberto Nakamoto, Attilio Fabbretti, Pohl Milón
Aminoglycoside antibiotics are widely used to treat infectious diseases. Among them, streptomycin and kanamycin (and derivatives) are of importance to battle multidrug-resistant (MDR) Mycobacterium tuberculosis. Both drugs bind the small ribosomal subunit (30S) and inhibit protein synthesis. Genetic, structural, and biochemical studies indicate that local and long-range conformational rearrangements of the 30S subunit account for this inhibition. Here, we use intramolecular FRET between the C- and N-terminus domains of the flexible IF3 to monitor real-time perturbations of their binding sites on the 30S platform...
December 13, 2016: Antibiotics
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