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Karen E Bowker, Alan R Noel, Sharon Tomaselli, Marie Attwood, Alasdair P MacGowan
Background: The pharmacodynamics of inhaled antimicrobials are poorly studied. Amikacin is being developed for inhalational therapy as BAY 41-6551. Objectives: We employed an in vitro pharmacokinetic model to study the pharmacokinetics/pharmacodynamics of amikacin. Methods: A dose-ranging design was used to establish fAUC/MIC and fCmax/MIC targets for static, -1 log drop and -2 log drop effects for strains of Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa...
March 19, 2018: Journal of Antimicrobial Chemotherapy
Seyed Mostafa Hasan Nasrollahi, Mohammad Ali Ghasemzadeh, Mohammad Reza Zolfaghari
The synthesis of heterocyclic compounds has been a topic of significant interest because of their broad applications. In this research an effective and eco-friendly approach for the synthesis 1,4-dihydropyridines has been developed via the four-component reactions of arylamines, acetylenedicarboxylates, aromatic aldehydes and ethyl acetoacetate in the presence of Fe3O4@SiO2@OSO3H nanocomposite under solvent-free conditions. The advantages of this method involve the green reaction conditions, simple workup, broad substrates, excellent yields and the reuse of the nanocatalyst...
March 2018: Acta Chimica Slovenica
Cuc Thi Thu Ngo, Leonard S Fishman, P Emile Rossouw, Hongyue Wang, Omar Said
OBJECTIVE: To determine the usefulness of panoramic radiographs in determining the labio-palatal position of maxillary impacted canines (MICs) and root resorption of permanent incisors on cone-beam computed tomography (CBCT) in correlation with the mesiodistal position of MICs on panoramic radiographs. MATERIALS AND METHODS: This retrospective radiographic study reviewed 64 patients with 86 MICs. Subjects were divided into two groups: group I (<15 years old) and group II (>15 years old)...
March 21, 2018: Angle Orthodontist
Irene Galani, Konstantina Nafplioti, Marianthi Chatzikonstantinou, Maria Souli
PURPOSE: The aim of this study was to evaluate the in vitro activity of double-carbapenem combinations against OXA-48-producing Klebsiella pneumoniae clinical isolates. METHODOLOGY: Double combinations of ertapenem, meropenem and imipenem were evaluated for synergy and bactericidal activity using the time-kill methodology. All antibiotics were tested at 10 mg l-1 and at a sub-inhibitory concentration of 0.5× minimum inhibitory concentration (MIC) for isolates with a carbapenem MIC≤8 mg l-1 ...
March 21, 2018: Journal of Medical Microbiology
Rossana de Aguiar Cordeiro, Ewerton Weslley Caracas Cedro, Ana Raquel Colares Andrade, Rosana Serpa, Antonio José de Jesus Evangelista, Jonathas Sales de Oliveira, Vandbergue Santos Pereira, Lucas Pereira Alencar, Patrícia Bruna Leite Mendes, Bárbara Cibelle Soares Farias, Vânia Maria Maciel Melo, Zoilo Pires de Camargo, Débora de Souza Collares Maia Castelo-Branco, Raimunda Sâmia Nogueira Brilhante, José Júlio Costa Sidrim, Marcos Fábio Gadelha Rocha
The present study aimed to investigate the inhibitory effect of a bacterial biosurfactant (TIM96) on clinical strains of Trichosporon. Additionally, the effect of TIM96 on the ergosterol content, cell membrane integrity, and the hydrophobicity of planktonic cells was assessed. The inhibitory activity of TIM96 against Trichosporon biofilms was evaluated by analyzing metabolic activity, biomass and morphology. MIC values ranged from 78.125 to 312.5 μg ml-1 for TIM96; time-kill curves revealed that the decline in the number of fungal cells started after incubation for 6 h with TIM96 at both MIC and 2×MIC...
March 21, 2018: Biofouling
Priya Kapoor, Philip Murphy
Objectives: To evaluate the effect of antibiotic combination therapy versus single therapy against cystic fibrosis strains of Pseudomonas aeruginosa identified as common and rare among patient groups in different Irish hospitals. Methods: This study compares the susceptibility profiles of P. aeruginosa isolates from different cystic fibrosis (CF) clinics in Ireland, collected from 2004-2005. Strains were recovered in small numbers and typed by pulsed-field gel electrophoresis...
March 2018: Heliyon
Abigail L Goodman, Shawn R Lockhart, Colleen B Lysen, Lars F Westblade, Carey-Ann D Burnham, Eileen M Burd
We present two cases of keratitis due to Metarhizium anisopliae in geographically separated areas of the United States. The isolates were microscopically similar but morphologically different and were identified by ribosomal DNA sequencing. Both isolates had low minimum inhibitory concentration (MIC) values to caspofungin and micafungin, but high MIC values to amphotericin B. The morphologic and antifungal susceptibility differences between the two isolates indicate possible polyphylogeny of the group.
September 2018: Medical Mycology Case Reports
A Gramegna, B C Millar, F Blasi, J S Elborn, D G Downey, J E Moore
INTRODUCTION: Pulmonary exacerbations in people with Cystic Fibrosis (CF), with chronic Gram-negative pathogens, are associated with reduced survival. These pathogens are usually treated with repeated courses of systemic antibiotics. However there is a linked emergence of multidrug resistant (MDR) pathogens. Ceftolozane/tazobactam is a new cephalosporin/beta-lactamase inhibitor combination that has been demonstrated to have good activity against MDR Pseudomonas aeruginosa. MATERIAL & METHODS: In this study ceftolozane/tazobactam was compared to other commonly used intravenous antibiotics against 193 non-fermenting Gram-negative bacteria isolated from CF sputum specimens, including P...
March 17, 2018: Journal of Global Antimicrobial Resistance
Matthew E Falagas, Tilemachos Skalidis, Konstantinos Z Vardakas, Georgios L Voulgaris, Georgios Papanikolaou, Nicholas Legakis
BACKGROUND: TP-6076 is a synthetic fluorocycline antibiotic that inhibits bacterial protein synthesis. METHODS: Carbapenem-resistant Acinetobacter baumannii clinical isolates from 13 Greek hospitals were tested for susceptibility to TP-6076 and comparator antibiotics. Broth microdilution plates were used to determine minimum inhibitory concentration (MIC) values. RESULTS: 121 A. baumannii non-duplicate isolates were tested. The MIC50 and MIC90 of TP-6076 were 0...
March 17, 2018: International Journal of Antimicrobial Agents
Jacqueline M Zaengle-Barone, Abigail C Jackson, David M Besse, Bradford Becken, Mehreen Arshad, Patrick C Seed, Katherine J Franz
The unabated rise in bacterial resistance to conventional antibiotics, coupled with collateral damage to normal flora incurred by overuse of broad-spectrum antibiotics, necessitates the development of new antimicrobials targeted against pathogenic organisms. Here, we explore the antibacterial outcomes and mode of action of a prochelator that exploits the production of β-lactamase enzymes by drug-resistant bacteria to convert a non-toxic compound into a metal-binding antimicrobial agent directly within the microenvironment of pathogenic organisms...
March 20, 2018: ACS Infectious Diseases
Maja Cindrić, Mihaela Perić, Marijeta Kralj, Irena Martin-Kleiner, Marie-Hélène David-Cordonnier, Hana Čipčić Paljetak, Mario Matijašić, Donatella Verbanac, Grace Karminski-Zamola, Marijana Hranjec
Novel nitro (3a-3f)- and amino (4a-4f and 5a-5f)-substituted 2-benzimidazolyl and 2-benzothiazolyl benzo[b]thieno-2-carboxamides were designed and synthesized as potential antibacterial agents. The antibacterial activity of these compounds has been evaluated against Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and Gram-negative bacteria (Escherichia coli and Moraxella catarrhalis). The most promising antibacterial activity was observed for the nitro- and amino-substituted benzimidazole derivatives 3a, 4a, 5a and 5b with MICs 2-8 [Formula: see text]...
March 20, 2018: Molecular Diversity
Ana S Oliveira, José Martinez-de-Oliveira, Gilbert G G Donders, Rita Palmeira-de-Oliveira, Ana Palmeira-de-Oliveira
As an opportunistic fungal pathogen Candida spp. has the ability to form biofilms. The most prescribed drugs for Candida infections, azoles, have shown to be less effective when biofilms are present. In addition, increasing treatment costs and the fact that most prescribed antifungal drugs have only fungistatic activity justify the search for new treatment strategies. One promising approach is third generation antidepressants, selective serotonin re-uptake inhibitors (SSRIs), because of their proven antifungal activity against several Candida spp...
March 19, 2018: Medical Microbiology and Immunology
Tang Gao, Hongliang Zeng, Huan Xu, Feng Gao, Wei Li, Shengwang Zhang, Yi Liu, Guifang Luo, Mingdan Li, Dejian Jiang, Zhigao Chen, Yong Wu, Wei Wang, Wenbin Zeng
Background: Increasing bacterial infections as well as a rise in bacterial resistance call for the development of novel and safe antimicrobial agents without inducing bacterial resistance. Nanoparticles (NPs) present some advantages in treating bacterial infections and provide an alternative strategy to discover new antibiotics. Here, we report the development of novel self-assembled fluorescent organic nanoparticles ( FONs ) with excellent antibacterial efficacy and good biocompatibility. Methods: Self-assembly of 1-(12-(pyridin-1-ium-1-yl)dodecyl)-4-(1,4,5-triphenyl-1H-imidazol-2-yl)pyridin-1-ium (TPIP) in aqueous solution was investigated using dynamic light scattering (DLS) and transmission electron microscopy (TEM)...
2018: Theranostics
Kieu-Nhi Tran, Michael J Rybak
Background: Increasing utilization of vancomycin due to the high prevalence of methicillin-resistant S. aureus (MRSA) infections has lead to the emergence of vancomycin-intermediate S. aureus (VISA) and heterogeneous VISA (hVISA). In vitro data suggest the potential for potent synergy between several beta-lactams and vancomycin. The objective of this study is to evaluate the synergy between beta-lactams and vancomycin against MRSA that is vancomycin susceptible, vancomycin susceptible Staphylococcus aureus (VSSA), hVISA, and VISA...
March 19, 2018: Antimicrobial Agents and Chemotherapy
Andrew M Stoessel, Cory M Hale, Robert W Seabury, Christopher D Miller, Jeffrey M Steele
OBJECTIVE: This study aimed to assess the impact of area under the curve (AUC)-based vancomycin monitoring on pharmacist-initiated dose adjustments after transitioning from a trough-only to an AUC-based monitoring method at our institution. METHODS: A retrospective cohort study of patients treated with vancomycin for complicated methicillin-resistant Staphylococcus aureus (MRSA) infection between November 2013 and December 2016 was conducted. The frequency of pharmacist-initiated dose adjustments was assessed for patients monitored via trough-only and AUC-based approaches for trough ranges: 10 to 14...
January 1, 2018: Journal of Pharmacy Practice
Stefanie Gerson, Jennifer Nowak, Esther Zander, Julia Ertel, Yurong Wen, Oleg Krut, Harald Seifert, Paul G Higgins
Objectives: To investigate the mechanisms of tigecycline resistance in isogenic Acinetobacter baumannii isolate pairs as well as 65 unique clinical A. baumannii isolates obtained during the MagicBullet clinical trial from Greece, Italy and Spain. Methods: A. baumannii isolates were subjected to WGS and the regulatory genes of resistance-nodulation-cell division (RND)-type efflux pumps were analysed. MICs were determined by agar dilution and the expression of RND-type efflux pumps was measured by semi-quantitative RT-PCR...
March 14, 2018: Journal of Antimicrobial Chemotherapy
Yoshinori Sato, Yuka Unno, Tsuneyuki Ubagai, Yasuo Ono
We investigated the numbers of planktonic and biofilm cells and the expression levels of genes encoding efflux pumps and biofilm-related proteins in 10 clinical isolates of multi-drug resistant Acinetobacter baumannii (MDRA) as well as in its standard strain ATCC 19606 in the presence of colistin (CST), polymyxin B (PMB), minomycin (MIN), and tigecycline (TGC) at their respective sub-MICs. The number of planktonic and biofilm cells of ATCC 19606 decreased in the presence of all aforementioned antibiotics in a dose-dependent manner...
2018: PloS One
Yong Liu, Lijian Ding, Fang Fang, Shan He
One novel 7-membered lactone derivative, penicillilactone A (1), together with two known compounds, rugulosin A (2) and rugulosin (3) were isolated from the sponge-derived fungus Penicillium sp. LS54. Their structures were elucidated on the basis of spectroscopic analysis and comparison with literature data. Remarkably, penicillilactone A (1) is the first natural product containing a 7-membered lactone ring fused with a furan core. Penicillilactone A (1) exhibited moderate antibacterial activity against aquatic pathogen Vibrio harveyi with an MIC value of 8 μg/mL...
March 19, 2018: Natural Product Research
Jinzhong Xu, Peng Liu, Xinyang Li, Lishe Gan, Pinmei Wang
Four novel stemphol derivatives, pleosporols A-D (1, 2 and mixture of 3 and 4) together with known compounds stemfolones (mixture of 5 and 6), stemphol (7) were isolated from a marine fungus Pleospora sp. (PO4) derived from the gut of marine isopod Ligia oceanica. The planar structures of novel compounds were elucidated on the basis of mass and NMR spectral analysis. The stereo-chemistries of 1-2 were determined by CD spectra, NOESY data, coupling constants analysis and modified Mosher's method while the absolute configurations of 3-6 were not clear...
March 19, 2018: Natural Product Research
Zheng Cui, Xiachang Wang, Stefan Koppermann, Jon S Thorson, Christian Ducho, Steven G Van Lanen
Muraymycins are nucleoside antibiotics isolated from Streptomyces sp. NRRL 30471 and several mutant strains thereof that were generated by random, chemical mutagenesis. Reinvestigation of two mutant strains using new media conditions led to the isolation of three new muraymycin congeners, named B8, B9, and C6 (1-3), as well as a known muraymycin, C1. Structures of the compounds were elucidated by HRMS and 1D and 2D NMR spectroscopic analyses. Complete 2D NMR assignments for the known muraymycin C1 are also provided for the first time...
March 19, 2018: Journal of Natural Products
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