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Antibiotics

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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/28075393/acknowledgement-to-reviewers-of-antibiotics-in-2016
#7
EDITORIAL
Antibiotics Editorial Office
The editors of Antibiotics would like to express their sincere gratitude to the following reviewers  for assessing manuscripts in 2016.[...].
January 10, 2017: Antibiotics
https://www.readbyqxmd.com/read/27983678/quorum-sensing-and-the-use-of-quorum-quenchers-as-natural-biocides-to-inhibit-sulfate-reducing-bacteria
#8
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
#9
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
https://www.readbyqxmd.com/read/27827853/antimicrobial-usage-and-antimicrobial-resistance-in-animal-production-in-southeast-asia-a-review
#10
REVIEW
Nguyen T Nhung, Nguyen V Cuong, Guy Thwaites, Juan Carrique-Mas
Southeast Asia is an area of great economic dynamism. In recent years, it has experienced a rapid rise in the levels of animal product production and consumption. The region is considered to be a hotspot for infectious diseases and antimicrobial resistance (AMR). We reviewed English-language peer-reviewed publications related to antimicrobial usage (AMU) and AMR in animal production, as well as antimicrobial residues in meat and fish from 2000 to 2016, in the region. There is a paucity of data from most countries and for most bacterial pathogens...
November 2, 2016: Antibiotics
https://www.readbyqxmd.com/read/27740593/pectocin-m1-pcam1-inhibits-escherichia-coli-cell-growth-and-peptidoglycan-biosynthesis-through-periplasmic-expression
#11
Dimitri Chérier, Sean Giacomucci, Delphine Patin, Ahmed Bouhss, Thierry Touzé, Didier Blanot, Dominique Mengin-Lecreulx, Hélène Barreteau
Colicins are bacterial toxins produced by some Escherichia coli strains. They exhibit either enzymatic or pore-forming activity towards a very limited number of bacterial species, due to the high specificity of their reception and translocation systems. Yet, we succeeded in making the colicin M homologue from Pectobacterium carotovorum, pectocin M1 (PcaM1), capable of inhibiting E. coli cell growth by bypassing these reception and translocation steps. This goal was achieved through periplasmic expression of this pectocin...
October 8, 2016: Antibiotics
https://www.readbyqxmd.com/read/27690121/resistance-to-%C3%AE-lactams-in-neisseria-ssp-due-to-chromosomally-encoded-penicillin-binding-proteins
#12
REVIEW
André Zapun, Cécile Morlot, Muhamed-Kheir Taha
Neisseria meningitidis and Neisseria gonorrhoeae are human pathogens that cause a variety of life-threatening systemic and local infections, such as meningitis or gonorrhoea. The treatment of such infection is becoming more difficult due to antibiotic resistance. The focus of this review is on the mechanism of reduced susceptibility to penicillin and other β-lactams due to the modification of chromosomally encoded penicillin-binding proteins (PBP), in particular PBP2 encoded by the penA gene. The variety of penA alleles and resulting variant PBP2 enzymes is described and the important amino acid substitutions are presented and discussed in a structural context...
September 28, 2016: Antibiotics
https://www.readbyqxmd.com/read/27690120/discrepancy-in-vancomycin-auc-mic-ratio-targeted-attainment-based-upon-the-susceptibility-testing-in-staphylococcus-aureus
#13
Seenae Eum, Robert L Bergsbaken, Craig L Harvey, J Bryan Warren, John C Rotschafer
This study demonstrated a statistically significant difference in vancomycin minimum inhibitory concentration (MIC) for Staphylococcus aureus between a common automated system (Vitek 2) and the E-test method in patients with S. aureus bloodstream infections. At an area under the serum concentration time curve (AUC) threshold of 400 mg∙h/L, we would have reached the current Infectious Diseases Society of America (IDSA)/American Society of Health System Pharmacists (ASHP)/Society of Infectious Diseases Pharmacists (SIDP) guideline suggested AUC/MIC target in almost 100% of patients while using the Vitek 2 MIC data; however, we could only generate 40% target attainment while using E-test MIC data (p < 0...
September 27, 2016: Antibiotics
https://www.readbyqxmd.com/read/27669322/the-peptidoglycan-pattern-of-staphylococcus-carnosus-tm300-detailed-analysis-and-variations-due-to-genetic-and-metabolic-influences
#14
Julia Deibert, Daniel Kühner, Mark Stahl, Elif Koeksoy, Ute Bertsche
The Gram-positive bacterium Staphylococcus carnosus (S. carnosus) TM300 is an apathogenic staphylococcal species commonly used in meat starter cultures. As with all Gram-positive bacteria, its cytoplasmic membrane is surrounded by a thick peptidoglycan (PGN) or murein sacculus consisting of several layers of glycan strands cross-linked by peptides. In contrast to pathogenic staphylococci, mainly Staphylococcus aureus (S. aureus), the chemical composition of S. carnosus PGN is not well studied so far. UPLC/MS analysis of enzymatically digested S...
September 23, 2016: Antibiotics
https://www.readbyqxmd.com/read/27669321/the-novel-aminomethylcycline-omadacycline-has-high-specificity-for-the-primary-tetracycline-binding-site-on-the-bacterial-ribosome
#15
Corina G Heidrich, Sanya Mitova, Andreas Schedlbauer, Sean R Connell, Paola Fucini, Judith N Steenbergen, Christian Berens
Omadacycline is an aminomethylcycline antibiotic with potent activity against many Gram-positive and Gram-negative pathogens, including strains carrying the major efflux and ribosome protection resistance determinants. This makes it a promising candidate for therapy of severe infectious diseases. Omadacycline inhibits bacterial protein biosynthesis and competes with tetracycline for binding to the ribosome. Its interactions with the 70S ribosome were, therefore, analyzed in great detail and compared with tigecycline and tetracycline...
September 22, 2016: Antibiotics
https://www.readbyqxmd.com/read/27649253/reconsultation-and-antimicrobial-treatment-of-urinary-tract-infection-in-male-and-female-patients-in-general-practice
#16
Meera Tandan, Sinead Duane, Martin Cormican, Andrew W Murphy, Akke Vellinga
Current antimicrobial prescribing guidelines indicate that male and female patients with urinary tract infections (UTIs) should be treated with same antimicrobials but for different durations. The aim of this study was to explore the differences in reconsultations and antimicrobial prescribing for UTI for both males and females. A total of 2557 adult suspected UTI patients participating in the Supporting the Improvement and Management of Prescribing for urinary tract infection (SIMPle) study from 30 general practices were analyzed...
September 15, 2016: Antibiotics
https://www.readbyqxmd.com/read/27626453/the-search-for-herbal-antibiotics-an-in-silico-investigation-of-antibacterial-phytochemicals
#17
Mary Snow Setzer, Javad Sharifi-Rad, William N Setzer
Recently, the emergence and spread of pathogenic bacterial resistance to many antibiotics (multidrug-resistant strains) have been increasing throughout the world. This phenomenon is of great concern and there is a need to find alternative chemotherapeutic agents to combat these antibiotic-resistant microorganisms. Higher plants may serve as a resource for new antimicrobials to replace or augment current therapeutic options. In this work, we have carried out a molecular docking study of a total of 561 antibacterial phytochemicals listed in the Dictionary of Natural Products, including 77 alkaloids (17 indole alkaloids, 27 isoquinoline alkaloids, 4 steroidal alkaloids, and 28 miscellaneous alkaloids), 99 terpenoids (5 monoterpenoids, 31 sesquiterpenoids, 52 diterpenoids, and 11 triterpenoids), 309 polyphenolics (87 flavonoids, 25 chalcones, 41 isoflavonoids, 5 neoflavonoids, 12 pterocarpans, 10 chromones, 7 condensed tannins, 11 coumarins, 30 stilbenoids, 2 lignans, 5 phenylpropanoids, 13 xanthones, 5 hydrolyzable tannins, and 56 miscellaneous phenolics), 30 quinones, and 46 miscellaneous phytochemicals, with six bacterial protein targets (peptide deformylase, DNA gyrase/topoisomerase IV, UDP-galactose mutase, protein tyrosine phosphatase, cytochrome P450 CYP121, and NAD⁺-dependent DNA ligase)...
September 12, 2016: Antibiotics
https://www.readbyqxmd.com/read/27598215/from-erythromycin-to-azithromycin-and-new-potential-ribosome-binding-antimicrobials
#18
REVIEW
Dubravko Jelić, Roberto Antolović
Macrolides, as a class of natural or semisynthetic products, express their antibacterial activity primarily by reversible binding to the bacterial 50S ribosomal subunits and by blocking nascent proteins' progression through their exit tunnel in bacterial protein biosynthesis. Generally considered to be bacteriostatic, they may also be bactericidal at higher doses. The discovery of azithromycin from the class of macrolides, as one of the most important new drugs of the 20th century, is presented as an example of a rational medicinal chemistry approach to drug design, applying classical structure-activity relationship that will illustrate an impressive drug discovery success story...
September 1, 2016: Antibiotics
https://www.readbyqxmd.com/read/27571111/the-membrane-steps-of-bacterial-cell-wall-synthesis-as-antibiotic-targets
#19
REVIEW
Yao Liu, Eefjan Breukink
Peptidoglycan is the major component of the cell envelope of virtually all bacteria. It has structural roles and acts as a selective sieve for molecules from the outer environment. Peptidoglycan synthesis is therefore one of the most important biogenesis pathways in bacteria and has been studied extensively over the last twenty years. The pathway starts in the cytoplasm, continues in the cytoplasmic membrane and finishes in the periplasmic space, where the precursor is polymerized into the peptidoglycan layer...
August 26, 2016: Antibiotics
https://www.readbyqxmd.com/read/27537922/exploring-experiences-of-delayed-prescribing-and-symptomatic-treatment-for-urinary-tract-infections-among-general-practitioners-and-patients-in-ambulatory-care-a-qualitative-study
#20
Sinead Duane, Paula Beatty, Andrew W Murphy, Akke Vellinga
"Delayed or back up" antibiotic prescriptions and "symptomatic" treatment may help to reduce inappropriate antibiotic prescribing for Urinary Tract Infections (UTI) in the future. However, more research needs to be conducted in this area before these strategies can be readily promoted in practice. This study explores General Practitioner (GP) and patient attitudes and experiences regarding the use of delayed or back-up antibiotic and symptomatic treatment for UTI. Qualitative face to face interviews with General Practitioners (n = 7) from one urban and one rural practice and telephone interviews with UTI patients (n = 14) from a rural practice were undertaken...
August 15, 2016: Antibiotics
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