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https://www.readbyqxmd.com/read/28103537/hybrids-of-thienopyrimidinones-and-thiouracils-as-anti-tubercular-agents-sar-and-docking-studies
#1
Mahesh M Pisal, Laxman U Nawale, Manoj D Patil, Sujit G Bhansali, Jayant M Gajbhiye, Dhiman Sarkar, Subhash P Chavan, Hanumant B Borate
A number of hybrid molecules containing thienopyrimidinones and thiouracil moieties were designed, synthesized and tested against Mycobacterium tuberculosis H37Ra wherein it was observed that the compounds 11-14 exhibited antitubercular activity in vitro (MIC 7.6-19.1 μg/mL, 12-35 μM) against dormant stage while the compound 15 exhibited antitubercular activity in vitro against dormant (MIC 23.4 μg/mL, 41 μM) as well as active (MIC 25.4 μg/mL, 45 μM) stage. Structural modifications of the compound 15 were carried out to study the structure-activity relationship and it was observed that the compound 18 exhibited antitubercular activity comparable to the compound 15...
January 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28103259/characterization-and-genetic-variation-of-vibrio-cholerae-isolated-from-clinical-and-environmental-sources-in-thailand
#2
Achiraya Siriphap, Pimlapas Leekitcharoenphon, Rolf S Kaas, Chonchanok Theethakaew, Frank M Aarestrup, Orasa Sutheinkul, Rene S Hendriksen
Cholera is still an important public health problem in several countries, including Thailand. In this study, a collection of clinical and environmental V. cholerae serogroup O1, O139, and non-O1/non-O139 strains originating from Thailand (1983 to 2013) was characterized to determine phenotypic and genotypic traits and to investigate the genetic relatedness. Using a combination of conventional methods and whole genome sequencing (WGS), 78 V. cholerae strains were identified. WGS was used to determine the serogroup, biotype, virulence, mobile genetic elements, and antimicrobial resistance genes using online bioinformatics tools...
2017: PloS One
https://www.readbyqxmd.com/read/28103015/antimicrobial-activity-ame-resistance-and-translation-inhibition-studies-of-anthraquinone-neomycin-conjugates
#3
Natalya N Degtyareva, Changjun Gong, Sandra Story, Nathanael Levinson, Adegboyega K Oyelere, Keith D Green, Sylvie Garneau-Tsodikova, Dev Priya Arya
The antibacterial effects of aminoglycosides are based on their association with the A-site of bacterial ribosomal RNA and interference with the translational process in the bacterial cell, causing cell death. The clinical use of aminoglycosides is complicated by resistance and side effects, some of which arise from their interactions with the human mitochondrial 12S rRNA and its deafness-associated mutations, C1494U and A1555G. We report a rapid assay that allows screening of aminoglycoside compounds to these classes of rRNAs...
January 19, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28102738/optimization-and-partial-characterization-of-intracellular-anticandidal-protein-from-aspergillus-giganteus-mtcc-8408-using-taguchi-doe
#4
Debashis Dutta, Mira Debnath Das
A new intracellular antifungal protein (afp) production with average molecular weight 24.3 kDa and yield of 0.65 ± 0.1 mg/gram dry cell weight (gdcw) of mycelia in submerged fermentation of Aspergillus giganteus MTCC 8408 was optimized. Taguchi's DOE (design of experiment) L27 orthogonal array (OA) was constructed using Qualitek-4 software with 8 most influensive factors namely, culture pH, temperature, slant age, inoculum volume, agitation and KH2PO4. Scanning electron microscopy (SEM) was used to correlate the effect of selected factors on fungal cell morphology and afp production...
January 19, 2017: Bioengineered
https://www.readbyqxmd.com/read/28101885/what-is-the-true-in%C3%A2-vitro-potency-of-oxytetracycline-for-the-pig-pneumonia-pathogens-actinobacillus-pleuropneumoniae-and-pasteurella-multocida
#5
L Dorey, S Hobson, P Lees
The pharmacodynamics of oxytetracycline was determined for pig respiratory tract pathogens, Actinobacillus pleuropneumoniae and Pasteurella multocida. Indices of potency were determined for the following: (i) two matrices, broth and pig serum; (ii) five overlapping sets of twofold dilutions; and (iii) a high strength starting culture. For A. pleuropneumoniae, minimum inhibitory concentration (MIC) was similar for the two matrices, but for P. multocida, differences were marked and significantly different. MIC and minimum bactericidal concentration (MBC) serum: broth ratios for A...
January 18, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28101253/2-chromon-3-yl-imidazole-derivatives-as-potential-antimicrobial-agents-synthesis-biological-evaluation-and-molecular-docking-studies
#6
Shweta Sharma, Vishal Sharma, Gurpreet Singh, Harpreet Kaur, Shubham Srivastava, Mohan Paul S Ishar
A series of novel 2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (4a-h) were synthesized by one pot condensation of substituted 3-formylchromones (1a-h), benzil (2) and ammonium acetate (3) in refluxing acetic acid at 110 °C under N2 atmosphere. Allylation of compounds 4a-h with allyl bromide in the presence of fused K2CO3 furnished N-allyl-2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (6a-h). The synthesized compounds were characterized spectroscopically and evaluated for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains by disc diffusion method...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28101153/upregulated-effects-of-mir-7-in-methicillin-resistant-staphylococcus-aureus
#7
Hong Zhang, Haiqing Li, Yan Liu, Qingyan Li, Yufang Bi, Guiqing Fang
The aim of the study was to investigate the characteristic function of the upregulated effects of miR-7 in methicillin-resistant Staphylococcus aureus (MRSA). After separating the MRSA in clinic, the expression of miR-7 mRNA was tested by reverse transcription polymerase chain reaction. The overexpression, inhibition of miR-7, and control group were established by plasmid in vitro. Following transfection of the bacterial strain, the effect of β-lactam antibiotics in minimum inhibitory concentration (MIC) was observed using the microporous dilution method, and antibacterial effects in vitro were observed using the dynamic growth curve method...
December 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28100900/paeonia-lactiflora-inhibits-cell-wall-synthesis-and-triggers-membrane-depolarization-in-candida-albicans
#8
Heung-Shick Lee, Younhee Kim
The fungal cell wall and cell membrane are main targets of antifungals. In this study, we report that antifungal activity of the ethanol extract from Paeonia lactiflora against Candida albicans is associated with synergistic action of preventing cell wall synthesis and changing membrane depolarization and permeability in C. albicans. First, the ethanol extract from P. lactiflora was involved in damaging the integrity of cell wall in C. albicans: In isotonic media, cell burst of C. albicans by the P. lactiflora ethanol extract could be restored, and minimum inhibitory concentration (MIC) of the P...
January 18, 2017: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28100598/molecular-and-matrix-assisted-laser-desorption-ionization-time-of-flight-mass-spectrometry-characterization-of-clinically-significant-melanized-fungi-in-india
#9
Ashutosh Singh, Pradeep Kumar Singh, Anil Kumar, Jagdish Chander, Geetika Khanna, Pradip Roy, Jacques F Meis, Anuradha Chowdhary
Melanized or black fungi are a heterogeneous group of fungi causing cutaneous to systemic diseases with high mortality. These fungi are rarely reported as agent of human infections primarily due to difficulties in their classical identification. In this study we examined using molecular methods and MALDI-TOF MS the diversity of melanized fungi (MF) isolated from patients in 19 medical centers in India. Overall, during a 4-year period, 718 (5.3%) clinical specimens yielded MF. Of these, 72 (10%) isolates had clinical significance and were identified primarily by sequencing the ITS and LSU regions...
January 18, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28100194/interspecies-transfer-of-vancomycin-erythromycin-and-tetracycline-resistance-among-enterococcus-species-recovered-from-agrarian-sources
#10
M Conwell, V Daniels, P J Naughton, J S G Dooley
BACKGROUND: Enterococci are now well recognised for their ability to transfer antibiotic resistance and for their association with nosocomial infections, but less is known regarding their relevance in the wider environment. Enterococcus faecalis and Enterococcus faecium were isolated from a range of agrarian associated sources (low-flow water, septic tank, poultry litter, high flow water, slurry/soil) and were assessed for latent ability to transfer antimicrobial resistance. RESULTS: The isolates were tested for phenotypic clumping in the presence of cell-free supernatant from other isolates...
January 18, 2017: BMC Microbiology
https://www.readbyqxmd.com/read/28099061/iodometric-and-molecular-detection-of-esbl-production-among-clinical-isolates-of-e-coli-fingerprinted-by-eric-pcr-the-first-egyptian-report-declares-the-emergence-of-e-coli-o25b-st131clone-harboring-blages
#11
Mohamed F El-Badawy, Wael M Tawakol, Ibrahim A Maghrabi, Moselhy S Mansy, Mohamed M Shohayeb, Mohammed S Ashour
The extensive use of β-lactam antibiotics has led to emergence and spread of extended-spectrum β-lactamases (ESBLs). This study was conducted to investigate the prevalence of 7 different ESBL genes (blaTEM, blaSHV, blaCTX-M, blaVEB, blaPER, blaGES, and blaOXA-10) and O25b-ST131 high-risk clone among 61 clinical isolates of Escherichia coli. Also, one broad-spectrum β-lactamase (blaOXA-1) was investigated. This study was also constructed to evaluate iodometric overlay method in detection of ESBL production...
January 18, 2017: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/28098790/synthesis-structure-and-antimicrobial-properties-of-novel-benzalkonium-chloride-analogues-with-pyridine-rings
#12
Bogumił Brycki, Izabela Małecka, Anna Koziróg, Anna Otlewska
Quaternary ammonium compounds (QACs) are a group of compounds of great economic significance. They are widely used as emulsifiers, detergents, solubilizers and corrosion inhibitors in household and industrial products. Due to their excellent antimicrobial activity QACs have also gained a special meaning as antimicrobials in hospitals, agriculture and the food industry. The main representatives of the microbiocidal QACs are the benzalkonium chlorides (BACs), which exhibit biocidal activity against most bacteria, fungi, algae and some viruses...
January 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28097898/two-approaches-to-the-use-of-benzo-c-1-2-oxaboroles-as-active-fragments-for-synthetic-transformation-of-clarithromycin
#13
Gennady B Lapa, Elena P Mirchink, Elena B Isakova, Maria N Preobrazhenskaya
Clarithromycin (active against Gram positive infections) and 1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborole derivatives (effective for Gram negative microbes) are the ligands of bacterial RNA. The antimicrobial activities of these benzoxaboroles linked with clarithromycin at 9 or 4″ position were compared. Two synthetic pathways for these conjugates were elaborated. First pathway explored the substitution of the C-9 carbonyl group of macrolactone's cycle via oxime linker, the second direction used the modification of the 4″-O-group of cladinose via the formation of carbamates of benzoxaboroles...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097041/effect-of-catechins-green-tea-extract-and-methylxanthines-in-combination-with-gentamicin-against-staphylococcus-aureus-and-pseudomonas-aeruginosa-combination-therapy-against-resistant-bacteria
#14
Bibi Sedigheh Fazly Bazzaz, Sahar Sarabandi, Bahman Khameneh, Hossein Hosseinzadeh
OBJECTIVES: Bacterial resistant infections have become a global health challenge and threaten the society's health. Thus, an urgent need exists to find ways to combat resistant pathogens. One promising approach to overcoming bacterial resistance is the use of herbal products. Green tea catechins, the major green tea polyphenols, show antimicrobial activity against resistant pathogens. The present study aimed to investigate the effect of catechins, green tea extract, and methylxanthines in combination with gentamicin against standard and clinical isolates of Staphylococcus aureus (S...
December 2016: Journal of Pharmacopuncture
https://www.readbyqxmd.com/read/28096686/peptide-consensus-sequence-determination-for-the-enhancement-of-the-antimicrobial-activity-and-selectivity-of-antimicrobial-peptides
#15
Ammar Almaaytah, Ya'u Ajingi, Ahmad Abualhaijaa, Shadi Tarazi, Nizar Alshar'i, Qosay Al-Balas
The rise of multidrug-resistant bacteria is causing a serious threat to the world's human population. Recent reports have identified bacterial strains displaying pan drug resistance against antibiotics and generating fears among medical health specialists that humanity is on the dawn of entering a post-antibiotics era. Global research is currently focused on expanding the lifetime of current antibiotics and the development of new antimicrobial agents to tackle the problem of antimicrobial resistance. In the present study, we designed a novel consensus peptide named "Pepcon" through peptide consensus sequence determination among members of a highly homologous group of scorpion antimicrobial peptides...
2017: Infection and Drug Resistance
https://www.readbyqxmd.com/read/28096545/thiazomycin-nocathiacin-and-analogs-show-strong-activity-against-clinical-strains-of-drug-resistant-mycobacterium-tuberculosis
#16
Sheo B Singh, Libo Xu, Peter T Meinke, Natalia Kurepina, Barry N Kreiswirth, David B Olsen, Katherine Young
Thiazolyl peptides are a class of natural products with potent Gram-positive antibacterial activities. Lack of aqueous solubility precluded this class of compounds from advancing to clinical evaluations. Nocathiacins and thiazomycins are sub-classes of thiazolyl peptides that are endowed with structural features amenable for chemical modifications. Semi-synthetic modifications of nocathiacin led to a series of analogs with improved water solubility, while retaining potency and antibacterial spectrum. We studied the activities of a selection of two natural products (nocathiacin and thiazomycin) as well as seven polar semi-synthetic analogs against twenty clinical strains of Mycobacterium tuberculosis with MDR phenotypes...
January 18, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28096164/pharmacodynamics-of-ceftaroline-plus-ampicillin-against-enterococcus-faecalis-in-an-in-vitro-pharmacokinetic-pharmacodynamic-model-of-simulated-endocardial-vegetations
#17
Brian J Werth, Laura M Shireman
The combination of ampicillin plus ceftaroline has been suggested to be more reliably synergistic against E. faecalis than ampicillin plus ceftriaxone using time-kill methods. The purpose of this study was to determine if this trend persists in a two-compartment-model of simulated endocardial vegetations(SEV) using clinically relevant pharmacokinetic exposures of these antimicrobials. Three clinically-derived E. faecalis strains were included in the study. The MICs of study antimicrobials were determined by broth microdilution...
January 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28096163/large-scale-evaluation-of-in-vitro-amphotericin-b-triazole-and-echinocandin-activity-against-coccidioides-species-from-united-states-institutions
#18
George R Thompson, Bridget M Barker, Nathan P Wiederhold
Large-scale testing of Coccidioides isolates has not previously been performed, nor has the frequency of clinical isolates with elevated amphotericin B or triazole MICs been evaluated. Coccidioides isolates (n=581) underwent antifungal susceptibility testing. Elevated MIC values were observed for: fluconazole (MIC ≥16 μg/ml, 37.3% of isolates; ≥32 μg/ml, 7.9%), itraconazole (1.0% ≥2 μg/ml), posaconazole (1.0% ≥1 μg/ml), and voriconazole (1.2% ≥2 μg/ml). However mould-active triazoles exhibited low MICs for the majority of isolates tested...
January 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28096160/determinants-of-antibacterial-spectrum-and-resistance-potential-of-the-elongation-factor-g-inhibitor-argyrin-b-in-key-gram-negative-pathogens
#19
Adriana K Jones, Angela L Woods, Kenneth T Takeoka, Xiaoyu Shen, Jun-Rong Wei, Ruth E Caughlan, Charles R Dean
Argyrins are natural products with antibacterial activity against Gram-negative pathogens such as P. aeruginosa, B. multivorans and S. maltophilia We previously showed that argyrin B targets elongation factor G (FusA). Here we show that Argyrin B activity against P. aeruginosa PAO1 (MIC = 8 μg/mL) was not affected by deletion of the MexAB-OprM, MexXY-OprM, MexCD-OprJ or MexEF-OprN efflux pumps. However, argyrin B induced expression of MexXY causing a slight but reproducible antagonism with the MexXY substrate antibiotic ciprofloxacin...
January 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28095918/anti-staphylococcal-activity-resulting-from-epithelial-lining-fluid-elf-concentrations-of-amikacin-inhale-administered-via-the-pulmonary-drug-delivery-system
#20
Islam M Ghazi, Mordechai Grupper, David P Nicolau
BACKGROUND: Amikacin inhale (BAY41-6551), a unique drug-device combination of a specially formulated drug solution and a pulmonary drug delivery system device (AMK-I) is currently under phase III study as an adjunctive therapy to IV antibiotics for the treatment of Gram-negative pneumonia in mechanically ventilated patients. While the epidemiology of nosocomial pneumonia is predominated by Gram-negative pathogens such as Pseudomonas aeruginosa and the Enterobacteriaceae, Staphylococcus aureus is increasingly recognized as a pathogen of concern for these pulmonary based infections...
January 17, 2017: Annals of Clinical Microbiology and Antimicrobials
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