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https://www.readbyqxmd.com/read/28645774/evaluation-of-selected-indian-medicinal-plants-for-antagonistic-potential-against-malassezia-spp-and-the-synergistic-effect-of-embelin-in-combination-with-ketoconazole
#1
Chandran Sivasankar, Subramanian Gayathri, James Prabhanand Bhaskar, Venkat Krishnan, Shunmugiah Karutha Pandian
The genus Malassezia comprises of extremely lipophilic yeasts secreting lipases as a vital factor for survival. They are emerging as opportunistic pathogens in medical microbiology and dermatology by causing recurring and recalcitrant infection. Combinatorial therapy is a constructive way to combat infectious diseases. In that prospect, totally 16 Indian medicinal plants were screened, among which a maximum degree of antimicrobial activity was ascertained in Embelia ribes. Subsequently embelin was identified as the bioactive principle with antagonistic potential by comparative antimicrobial assay and FTIR analysis...
June 20, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28645327/impact-of-growth-matrix-on-pharmacodynamics-of-antimicrobial-drugs-for-pig-pneumonia-pathogens
#2
Lucy Dorey, Peter Lees
BACKGROUND: The most widely used measure of potency of antimicrobial drugs is Minimum Inhibitory Concentration (MIC). MIC is usually determined under standardised conditions in broths formulated to optimise bacterial growth on a species-by-species basis. This ensures comparability of data between laboratories. However, differences in values of MIC may arise between broths of differing chemical composition and for some drug classes major differences occur between broths and biological fluids such as serum and inflammatory exudate...
June 23, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/28644704/numerical-analysis-of-time-dependent-inhibition-kinetics-comparison-between-rat-liver-microsomes-and-rat-hepatocyte-data-for-mechanistic-model-fitting
#3
Chuong Pham, Swati Nagar, Ken Korzekwa
Time dependent inhibition (TDI) may confound drug interaction predictions. Recently, models were generated for an array of TDI kinetic schemes using numerical analysis of microsomal assays. Additionally, a distinct terminal inactivation step was identified for certain mechanism based inhibitors (MBI) following reversible metabolite intermediate complex (MIC) formation. Longer hepatocyte incubations potentially allow analysis of slow TDI and terminal inactivation. In the experiments presented here, we compared the quality of TDI parameterization by numerical analysis between hepatocyte and microsomal data...
June 23, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28642934/evaluation-of-the-antibacterial-and-antifungal-properties-of-phragmanthera-capitata-sprengel-balle-loranthaceae-a-mistletoe-growing-on-rubber-tree-using-the-dilution-techniques
#4
Franklin Uangbaoje Ohikhena, Olubunmi Abosede Wintola, Anthony Jide Afolayan
The alarming increase in multidrug resistance of pathogenic microorganisms to conventional drugs in recent years has prompted the search for new leads in alternative remedies in natural products. Hence, this study was aimed at evaluating the antimicrobial properties of Phragmanthera capitata, a parasitic mistletoe growing on rubber trees. The in vitro antimicrobial activities of the acetone, methanol, ethanol, and aqueous extracts were investigated using five gram-negative and five gram-positive bacteria and four fungi...
2017: TheScientificWorldJournal
https://www.readbyqxmd.com/read/28634338/coumarin-benzimidazole-hybrids-as-a-potent-antimicrobial-agent-synthesis-and-biological-elevation
#5
L Ravithej Singh, Srinivasa Rao Avula, Sneha Raj, Akanksha Srivastava, Gopala Reddy Palnati, C K M Tripathi, Mukesh Pasupuleti, Koneni V Sashidhara
Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris...
June 21, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28630204/a-low-molecular-weight-alginate-oligosaccharide-disrupts-pseudomonal-microcolony-formation-and-enhances-antibiotic-effectiveness
#6
Manon F Pritchard, Lydia C Powell, Alison A Jack, Kate Powell, Konrad Beck, Hannah Florance, Julian Forton, Philip D Rye, Arne Dessen, Katja E Hill, David W Thomas
In chronic respiratory disease the formation of dense, 3-dimensional 'micro colonies' by Pseudomonas aeruginosa within the airway plays an important role in contributing to resistance to treatment. An in vitro biofilm model of pseudomonal microcolony formation using artificial sputum (AS) medium was established to study the effects of low molecular weight alginate oligomers (OligoG CF-5/20) on pseudomonal growth, microcolony formation and the efficacy of colistin. The studies employed clinical cystic fibrosis (CF) isolates (n=3) and reference non-mucoid and mucoid multi-drug resistant (MDR) CF isolates (n=7)...
June 19, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28626525/identification-of-better-pharmacokinetic-benzothiazinone-derivatives-as-new-antitubercular-agents
#7
Kai Lv, Xuefu You, Bin Wang, Zengquan Wei, Yun Chai, Bo Wang, Apeng Wang, Guocheng Huang, Mingliang Liu, Yu Lu
A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent in vitro activity (MIC < 0.15 μM) against the drug susceptive Mycobacterium tuberculosis H37Rv strain and two clinically isolated multidrug-resistant strains. Compounds 11l and 11m display acceptable safety, greater aqueous solubility, and better pharmacokinetic profiles than PBTZ169, suggesting their promising potential to be lead compounds for future antitubercular drug discovery...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28622712/evaluation-of-the-antibacterial-and-modulatory-potential-of-%C3%AE-bisabolol-%C3%AE-cyclodextrin-and-%C3%AE-bisabolol-%C3%AE-cyclodextrin-complex
#8
Fernanda de Sousa Oliveira, Thiago Sampaio de Freitas, Rafael Pereira da Cruz, Maria do Socorro Costa, Raimundo Luiz Silva Pereira, Lucindo José Quintans-Júnior, Tatianny de Araújo Andrade, Paula Dos Passos Menezes, Bruna Maria Hipólito de Sousa, Paula Santos Nunes, Mairim Russo Serafini, Irwin Rose Alencar de Menezes, Adriano Antunes de Souza Araújo, Henrique Douglas Melo Coutinho
The present study aimed to evaluate the antibacterial and modulatory potential of α-bisabolol, β-cyclodextrin and α-bisabolol/β-cyclodextrin complex. The minimum inhibitory concentration was determined through the broth microdilution technique using the bacterial strains: Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. The drugs norfloxacin, imipenem and gentamicin were used in the tests, and the compounds α-bisabolol and β-cyclodextrin; all the compounds were diluted in DMSO. To obtain the minimum inhibitory concentration (MIC) a serial microdilution of the substances in volumes corresponding to the sub-inhibitory concentration (MIC/8), and microdilution with the antibiotic until the penultimate well were performed...
June 12, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28621733/discovery-of-indeno-1-2-c-quinoline-derivatives-as-potent-dual-antituberculosis-and-anti-inflammatory-agents
#9
Chih-Hua Tseng, Chun-Wei Tung, Chen-Hsin Wu, Cherng-Chyi Tzeng, Yen-Hsu Chen, Tsong-Long Hwang, Yeh-Long Chen
A series of indeno[1,2-c]quinoline derivatives were designed, synthesized and evaluated for their anti-tuberculosis (anti-TB) and anti-inflammatory activities. The minimum inhibitory concentration (MIC) of the newly synthesized compound was tested against Mycobacterium tuberculosis H37RV. Among the tested compounds, (E)-N'-[6-(4-hydroxypiperidin-1-yl)-11H-indeno[1,2-c]quinolin-11-ylidene]isonicotino-hydrazide (12), exhibited significant activities against the growth of M. tuberculosis (MIC values of 0.96 μg/mL) with a potency approximately equal to that of isoniazid (INH), an anti-TB drug...
June 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28621597/pharmacokinetics-of-chloramphenicol-base-after-oral-administration-in-adult-horses
#10
Eva M McElligott, Carla S Sommardahl, Sherry K Cox
OBJECTIVE To determine the pharmacokinetics of chloramphenicol base after PO administration at a dose of SO mg/kg (22.7 mg/lb) in adult horses from which food was not withheld. DESIGN Prospective crossover study. ANIMALS 5 adult mares. PROCEDURES Chloramphenicol base (SO mg/kg) was administered PO to each horse, and blood samples were collected prior to administration (0 minutes) and at 5, 10, 15, and 30 minutes and 1, 2, 4, 8, and 12 hours thereafter. Following a washout period, chloramphenicol sodium succinate (25 mg/kg [11...
July 1, 2017: Journal of the American Veterinary Medical Association
https://www.readbyqxmd.com/read/28620888/design-of-isoniazid-smart-nanogel-by-gamma-radiation-induced-template-polymerization-for-biomedical-application
#11
Samia M Omar, Nabila A Maziad, Nourhan M El-Tantawy
PURPOSE: Preparation of Isoniazid (INH) loaded nanogel particles using gamma radiation as safe, simple, cheap and reproducible technique for promoting mycobacterial killing in a lower-dose system aiming in developing of drug resistance. METHODS: Polymeric pH-sensitive nanogels were prepared by gamma radiation-induced polymerization of Acrylic acid (AAc) or Itaconic acid (IA), in aqueous solution of polyvinylpyrrolidone (PVP), as template polymer. The prepared nanogels were utilized for encapsulation of INH...
June 15, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28619611/an-insight-into-selection-specificity-of-quinolone-resistance-determinants-within-enterobacteriaceae-family
#12
Nivedita Dasgupta, Deepjyoti Paul, Debadatta DharChanda, Birson Ingti, Dibyojyoti Bhattacharjee, Atanu Chakravarty, Amitabha Bhattacharjee
OBJECTIVES: Quinolone antimicrobials are frequently misused due to self-medication and suboptimal dose administration, leading to the development of resistance as well as treatment failure. The present study aimed to characterise plasmid-mediated quinolone resistance (PMQR) determinants and their genetic selection in the presence of quinolone stress within members of the Enterobacteriaceae. METHODS: A total of 209 non-duplicate Enterobacteriaceae isolates were collected from hospital and community health centres over the period July 2013 to June 2014...
June 12, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28611662/an-antifungal-mechanism-of-protolichesterinic-acid-from-the-lichen-usnea-albopunctata-lies-in-the-accumulation-of-intracellular-ros-and-mitochondria-mediated-cell-death-due-to-apoptosis-in-candida-tropicalis
#13
S N Kumar, C Mohandas
Candida species causes superficial and life-threatening systemic infections and are difficult to treat due to the resistance of these organism to various clinically used drugs. Protolichesterinic acid is a well-known lichen compound. Although the antibacterial activity of protolichesterinic acid has been reported earlier, the antifungal property and its mechanism of action are still largely unidentified. The goal of the present investigation is to explore the anticandidal activity and mechanism of action of protolichesterinic acid, especially against Candida tropicalis...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28607025/pharmacodynamic-evaluation-of-fosfomycin-against-e-coli-and-klebsiella-spp-from-urinary-tract-infections-and-the-influence-of-ph-on-fosfomycin-activities
#14
Nayara Helisandra Fedrigo, Josmar Mazucheli, James Albiero, Danielle Rosani Shinohara, Fernanda Gomes Lodi, Ana Cristina Dos Santos Machado, Sherwin K B Sy, Maria Cristina Bronharo Tognim
Fosfomycin is widely used for the treatment of uncomplicated urinary tract infection (UTI) and recently have been recommended for treating multidrug-resistant (MDR) gram-negative bacilli. Whether urine acidification can improve bacterial susceptibility to fosfomycin oral dosing regimen has not been analyzed. Minimal inhibitory concentration (MIC) was determined using agar dilution in pH 6.0 and 7.0 for 245 Gram negative bacterial isolates, consisting of 158 E. coli and 87 Klebsiella spp. which were collected from patients with UTI...
June 12, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28606047/design-synthesis-and-biological-evaluation-of-vanillin-hydroxamic-acid-derivatives-as-novel-peptide-deformylase-inhibitors
#15
Jian Gao, Shengzhi Qiu, Li Liang, Zhixiang Hao, Qianqian Zhou, Fanfan Wang, Jie Mou, Qisi Lin
BACKGROUND: Infectious disease is increasingly hampering human health, which challenge the discovery of new antibacterial target. Peptide deformylase (PDF), a metalloenzyme responsible for catalyzing the remove of the N-formyl group from nascent proteins, was considered as an important target in antibacterial drug discovery. OBJECTIVE: Reported here are the design, synthesis and biological evaluation of vanillin hydroxamic acid derivatives. METHOD AND RESULTS: Analysis of the structure-activity relationships lead to the discovery of compound 8, which exhibits promising antibacterial activity against Escherichia coli, Staphylococcus aureus, Aspergillus oryzae, and Aspergillus foetidus with the MIC value of 0...
June 12, 2017: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/28605982/chemical-composition-and-antifungal-activity-of-hedera-helix-leaf-ethanolic-extract
#16
Oana Roşca-Casian, Cristina Mircea, Laurian Vlase, Ana-Maria Gheldiu, Delia Tania Teuca, Marcel Pârvu
The 50% ethanol extract obtained from Hedera helix leaves was investigated regarding the presence and quantity of polyphenols, sterols and in vitro antifungal activity against phytopathogenic fungi. The chemical analysis revealed the presence of rutin, quercetin and kaempferol in the non-hydrolysed sample and quercetin and kaempferol in the hydrolysed sample and stigmasterol in the ivy leaf extract (nonhydrolysed sample). The antifungal activity against phytopathogenic fungi (Aspergillus niger, Botrytis cinerea, B...
June 2017: Acta Biologica Hungarica
https://www.readbyqxmd.com/read/28605490/adequate-plasma-drug-concentrations-suggest-that-amoxicillin-can-be-administered-by-continuous-infusion-using-elastomeric-pumps
#17
Lyne Arensdorff, Noémie Boillat-Blanco, Laurent Decosterd, Thierry Buclin, Serge de Vallière
Background: Elastomeric pumps can be useful for the administration of antibiotics in the outpatient setting. Objectives: To determine amoxicillin degradation in elastomeric pumps, as well as the effectiveness of amoxicillin treatment administered by elastomeric pumps. Methods: Antibiotic degradation was measured in elastomeric pumps filled with 6 g of amoxicillin in 240 mL of NaCl 0.9% by drawing samples at 12 h intervals when stored in the fridge for 48 h and when worn around the waist for 24 h...
June 12, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28603609/antimicrobial-susceptibility-of-clostridium-difficile-isolated-in-thailand
#18
Papanin Putsathit, Monthira Maneerattanaporn, Pipat Piewngam, Daniel R Knight, Pattarachai Kiratisin, Thomas V Riley
BACKGROUND: Exposure to antimicrobials is the major risk factor associated with Clostridium difficile infection (CDI). Paradoxically, treatment of CDI with antimicrobials remains the preferred option. To date, only three studies have investigated the antimicrobial susceptibility of C. difficile from Thailand, two of which were published in the 1990s. This study aimed to investigate the contemporary antibiotic susceptibility of C. difficile isolated from patients in Thailand. METHODS: A collection of 105 C...
2017: Antimicrobial Resistance and Infection Control
https://www.readbyqxmd.com/read/28600080/novel-pyridyl-nitrofuranyl-isoxazolines-show-antibacterial-activity-against-multiple-drug-resistant-staphylococcus-species
#19
Pietro Picconi, Priya Prabaharan, Jennifer L Auer, Stephanie Sandiford, Francesco Cascio, Madiha Chowdhury, Charlotte Hind, Matthew E Wand, J Mark Sutton, Khondaker M Rahman
A novel series of pyridyl nitrofuranyl isoxazolines were synthesized and evaluated for their antibacterial activity against multiple drug resistant (MDR) Staphylococcus strains. Compounds with piperazine linker between the pyridyl group and isoxazoline ring showed better activity when compared to compounds without the piperazine linker. 3-Pyridyl nitrofuranyl isoxazoline with a piperazine linker was found to be more active than corresponding 2-and 4-pyridyl analogues with MICs in the range of 4-32µg/mL against MDR Staphylococcus strains...
May 19, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28598307/exposure-to-sub-inhibitory-concentrations-of-gentamicin-ciprofloxacin-and-cefotaxime-induces-multidrug-resistance-and-reactive-oxygen-species-generation-in-meticillin-sensitive-staphylococcus-aureus
#20
Gargi Bhattacharya, Diganta Dey, Satadal Das, Abhijit Banerjee
PURPOSE: The role of antibiotics below their MIC in the development of bacterial drug resistance is becoming increasingly important. We investigated the effect of sub-MICs of bactericidal antibiotics on the susceptibility pattern of Staphylococcus aureus and evaluated the role of free radicals. METHODOLOGY: A total of 12 S. aureus strains were recovered from pus samples and their antibiograms determined. The test isolates were treated with sub-MIC levels of tetracycline, gentamicin, ciprofloxacin and cefotaxime...
June 2017: Journal of Medical Microbiology
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