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https://www.readbyqxmd.com/read/28544494/4-substituted-thieno-2-3-d-pyrimidines-as-potent-antibacterial-agents-rational-design-microwave-assisted-synthesis-biological-evaluation-and-molecular-docking-studies
#1
Rupinder K Gill, Harpreet Singh, Tilak Raj, Anuradha Sharma, Gagandeep Singh, Jitender Bariwal
In an attempt to discover a new class of antibacterial agents with improved efficacy and to overcome the drug resistant problems, some novel 4-substituted thieno[2,3-d]pyrimidines have been synthesized via microwave assisted methodology and evaluated for their in vitro antibacterial activity against various pathogenic bacterial strains. Compounds 12b and 13c showed the promising inhibitory potencies against S. aureus, B. subtilis, P. aeruginosa and E. coli with MICs ranging from 2 to 10 μg/ml. Compound 13c was also found to be highly potent against methicillin resistant S...
May 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28539745/effect-of-tamarindus-indica-l-and-manihot-esculenta-extracts-on-antibiotic-resistant-bacteria
#2
Zenon Machado Lima, Lenilson Santos da Trindade, Genelane Cruz Santana, Francine Ferreira Padilha, Marcelo da Costa Mendonça, Luiz Pereira da Costa, Jorge A López, Maria Lucila Hernández Macedo
BACKGROUND: The chemical composition of plants used in traditional medicine exhibits biologically active compounds, such as tannins, flavonoids, and alkaloids and becomes a promising approach to treat microbial infections, mainly with drug-resistant bacteria. OBJECTIVE: The aim of the present study was to evaluate the hydroethanolic leaf extracts of Tamarindus indica (tamarind) and Manihot esculenta (cassava) as antimicrobial potential against Pseudomonas aeruginosa clinical isolated and Methicillin-resistant Staphylococcus aureus...
April 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28539728/anti-quorum-sensing-activity-of-forsythia-suspense-on-chromobacterium-violaceum-and-pseudomonas-aeruginosa
#3
An Zhang, Wei-Hua Chu
BACKGROUND: Quorum sensing (QS) plays an important role in the production of virulence factors and pathogenicity in Pseudomonas aeruginosa, and the interruption of QS will be a hopeful pathway to combat bacterial infection. OBJECTIVE: In this study, we selected Forsythia suspense (Thunb.) Vahl from traditional Chinese herbal medicines for its anti-QS activity. MATERIALS AND METHODS: Anti-QS of F. suspense extracts (FSE) was monitored using the Chromobacterium violaceum 12472 bioassay...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28539723/antimicrobial-and-anti-inflammatory-effects-of-ethanol-extract-of-corylopsis-coreana-uyeki-flos
#4
Da-Eon Park, In-Soo Yoon, Jung-Eun Kim, Ji-Hye Seo, Jin-Cheol Yoo, Chun-Sik Bae, Chang-Dai Lee, Dae-Hun Park, Seung-Sik Cho
BACKGROUND: Corylopsis coreana Uyeki (Hamamelidaceae) is a medicinal plant cultivated in Northeast Asia. Previously, we have reported that an ethanol extract of Corylopsis coreana Uyeki flos (ECCF) contains four active compounds with antioxidant activity. OBJECTIVE: The aim of this study was to investigate the antimicrobial spectrum against infectious bacteria and anti-inflammatory effect of ECCF in a mouse model of acute local inflammation. MATERIALS AND METHODS: In vitro antimicrobial susceptibility was evaluated using standard plate assay technique...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28535203/are-moxifloxacin-and-levofloxacin-equally-effective-to-treat-xdr-tuberculosis
#5
Thomas Maitre, Grégoire Petitjean, Aurélie Chauffour, Christine Bernard, Najoua El Helali, Vincent Jarlier, Florence Reibel, Pascal Chavanet, Alexandra Aubry, Nicolas Veziris
Background: : Moxifloxacin retains partial activity against some fluoroquinolone-resistant mutants of Mycobacterium tuberculosis . Levofloxacin is presumed to be as active as moxifloxacin against drug-susceptible tuberculosis and to have a better safety profile. Objectives: : To compare the in vivo activity of levofloxacin and moxifloxacin against M. tuberculosis strains with various levels of fluoroquinolone resistance. Methods: BALB/c mice were intravenously infected with 10 6 M...
May 23, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28533240/heterocycle-thiazole-compounds-exhibit-antifungal-activity-through-increase-in-the-production-of-reactive-oxygen-species-in-cryptococcus-neoformans-cryptococcus-gattii-species-complex
#6
Nívea Pereira de Sá, Caroline Miranda de Lima, Cleudiomar Inácio Lino, Paulo Jorge Sanches Barbeira, Ludmila de Matos Baltazar, Daniel Assis Santos, Renata Barbosa de Oliveira, Eleftherios Mylonakis, Beth Burgwyn Fuchs, Susana Johann
Human cryptococcosis can occur as a primary or opportunistic infection and develops as an acute, sub-acute, or chronic systemic infection, involving different organs of the host. Given the limited therapeutic options and the occasional resistance to fluconazole, there is a need to develop novel drugs for the treatment of cryptococcosis. In this report, we describe promising thiazoles 1, 2, 3, and 4 and explore their possible modes of action against Cryptococcus. To this end, we show evidence of interference in the Cryptococcus antioxidant system...
May 22, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28533232/potentiation-of-antibiotic-activity-by-a-novel-cationic-peptide-potency-and-spectrum-of-activity-of-spr741
#7
David Corbett, Andrew Wise, Tara Langley, Kirsty Skinner, Emily Trimby, Stephen Birchall, Alain Dorali, Stephanie Sandiford, Jennifer Williams, Peter Warn, Martti Vaara, Troy Lister
Novel approaches to the treatment of multi-drug resistant Gram-negative bacterial infections are urgently required. One approach is to potentiate the efficacy of existing antibiotics whose spectrum of activity is limited by the permeability barrier presented by the Gram-negative outer membrane. Cationic peptides derived from polymyxin B have been used to permeabilize the outer membrane, granting antibiotics that would otherwise be excluded access to their targets. We assessed the in vitro efficacy of combinations of SPR741 with conventional antibiotics against Escherichia coli, Klebsiella pneumoniae, and Acinetobacter baumannii Of 35 antibiotics tested, the MICs of eight were reduced 32- to 8,000-fold against E...
May 22, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28530541/synthesis-of-new-antibacterial-cubane-based-nanocomposite-and-its-application-in-combination-cancer-therapy
#8
Elham Zakerzadeh, Roya Salehi, Mehrdad Mahkam
BACKGROUND: The need for therapeutically effective anticancer drug delivery systems constantly persuades researchers to explore novel strategies. OBJECTIVE: In this study a novel cubane based antibacterial nanocomposite was tailored as dual chemotherapy drug delivery vesicle in order to increase the therapeutic outcome in cancer therapy. METHOD: The physico-chemical characterization of engineered nanocarrier was assessed by Fourier transforms infrared spectroscopy (FTIR), Hydrogen nuclear magnetic resonance spectroscopy (1H NMR), Thermogravimetric analysis (TGA), and Field emission scanning electron microscopy-energy dispersive using X-ray (FESEM-EDX)...
May 22, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28529027/management-of-postneurosurgical-meningitis-narrative-review
#9
REVIEW
Khetam Hussein, Roni Bitterman, Ben Shofty, Mical Paul, Ami Neuberger
BACKGROUND: Infections complicating neurosurgery pose unacceptable mortality and morbidity. AIMS: To summarize what is known about the epidemiology, diagnosis and treatment of post-neurosurgical meningitis (PNM). SOURCES: PubMed, references of identified studies and reviews, and personal experience when evidence was lacking. CONTENT: The incidence and pathogen distribution of PNM is highly variable. A shift towards Gram-negative bacteria has been observed with use of antibiotic prophylaxis and antibiotic-coated devices directed mainly against Gram-positive bacteria...
May 18, 2017: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/28528487/role-of-medicines-of-unknown-identity-in-adverse-drug-reaction-related-hospitalizations-in-developing-countries-evidence-from-a-cross-sectional-study-in-a-teaching-hospital-in-the-lao-people-s-democratic-republic
#10
Céline Caillet, Chanvilay Sichanh, Gaëtan Assemat, Myriam Malet-Martino, Agnès Sommet, Haleh Bagheri, Noudy Sengxeu, Niphonh Mongkhonmath, Mayfong Mayxay, Lamphone Syhakhang, Maryse Lapeyre-Mestre, Paul N Newton, Anne Roussin
INTRODUCTION: The health dangers of medicines of unknown identity (MUIs) [loose pharmaceutical units repackaged in individual bags without labelling of their identity] have been suspected in L/MICs. Using visual and analytical tools to identify MUIs, we investigated the frequency of, and factors associated with, adverse drug reaction (ADR)-related hospitalizations in a central hospital in Vientiane Capital, Lao People's Democratic Republic (PDR). METHODS: All unplanned admissions, except for acute trauma and intentional overdose, were prospectively recorded during a 7-week period in 2013, leading to include 453 adults hospitalized for ≥24 h...
May 20, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/28526056/the-blood-schizonticidal-activity-of-tafenoquine-makes-an-essential-contribution-to-its-prophylactic-efficacy-in-nonimmune-subjects-at-the-intended-dose-200%C3%A2-mg
#11
REVIEW
Geoffrey Dow, Bryan Smith
Tafenoquine (TQ) is an 8-aminoquinoline anti-malarial being developed for malaria prophylaxis. It has been generally assumed that TQ, administered prophylactically, acts primarily on the developing exoerythrocytic stages of malaria parasites (causal prophylaxis), and that polymorphisms in metabolic enzymes thought to impact the activity of other 8-aminoquinolines also inhibit this property of TQ. Furthermore, it has been suggested that a diagnostic test for CYP2D6 metabolizer status might be required. In field studies in which metabolic status was not an exclusion criteria, TQ has been shown to exhibit similar prophylactic efficacy as blood schizonticidal drugs (mefloquine)...
May 19, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28524024/-efficacy-and-safety-of-colistimethate-sodium-in-critical-patients-an-in-vitro-study-by-using-of-monte-carlo-simulation
#12
Aijun Pan, Qing Mei, Tianjun Yang, Xiaolan Gao, Huaiwei Lu, Ying Ye, Jiabin Li, Bao Liu
OBJECTIVE: To evaluate the efficacy and safety of colistimethate sodium (CMS) for the treatment of critical patients infected by pan-drug resistant Acinetobacter baumannii (PDR-AB) or pan-drug resistant Pseudomonas aeruginosa (PDR-PA). METHODS: 321 isolates of PDR-AB and 204 isolates of PDR-PA from critical patients admitted to 35 intensive care units (ICUs) of grade two or above were collected from the Anhui Antimicrobial Resistance Investigation Net (AHARIN) program from September 2012 to September 2015, while the minimal inhibitory concentrations (MIC) of colistin were determined by the E-test...
May 2017: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue
https://www.readbyqxmd.com/read/28523106/discovery-of-fluorine-containing-benzoxazinyl-oxazolidinones-for-the-treatment-of-multidrug-resistant-tuberculosis
#13
Hongyi Zhao, Yu Lu, Li Sheng, Zishuo Yuan, Bin Wang, Weiping Wang, Yan Li, Chen Ma, Xiaoliang Wang, Dongfeng Zhang, Haihong Huang
A novel series of fluorine-containing benzoxazinyl-oxazolidinones were designed and synthesized as antidrug-resistant tuberculosis agents possessing good activity and improved pharmacokinetic profiles. Compound 21 exhibited not only outstanding in vitro activity with a MIC value of 0.25-0.50 μg/mL against drug-susceptible H37Rv strain and two clinically isolated drug-resistant Mycobacterium tuberculosis strains, but also acceptable in vitro ADME/T properties. Moreover, this compound displayed excellent mouse pharmacokinetic profiles with an oral bioavailability of 102% and a longer elimination half-life of 4...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28522372/effective-antimicrobial-activity-of-a-peptide-mutant-cbf-14-2-against-penicillin-resistant-bacteria-based-on-its-unnatural-amino-acids
#14
Wei Kang, Hanhan Liu, Lingman Ma, Mengxiao Wang, Shanshan Wei, Pengbo Sun, Meiling Jiang, Min Guo, Changlin Zhou, Jie Dou
Broad spectrum activities, a unique mode of actions and rare resistant variants make antimicrobial peptide (AMP) a potential alternative to antibiotics. However, AMPs still have limitations in clinical development due to their physiological stability, toxicity and manufacturing costs. Cbf-14, derived from cathelicidin-BF has been proven to be effective against drug-resistant bacteria. Herein, a series of Cbf-14 mutants were designed to overcome these limitations. Design strategies included substitutions of lysine (Lys) or leucine (Leu) with similar residues such as ornithine (Orn) and norleucine (Ile), which are unnatural amino acids, to generate AMPs with enhanced therapeutic potential...
May 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28522362/susceptibility-of-bacterial-vaginosis-bv-associated-bacteria-to-secnidazole-compared-to-metronidazole-tinidazole-and-clindamycin
#15
Melinda A B Petrina, Lisa A Cosentino, Lorna K Rabe, Sharon L Hillier
Secnidazole, a 5-nitroimidazole with a longer half-life, is structurally related to metronidazole and tinidazole. For treatment of bacterial vaginosis (BV), secnidazole is a suitable single-dose oral drug having a longer serum half-life than metronidazole. The objective of this study was to evaluate the antimicrobial susceptibility of vaginal isolates of facultative and anaerobic bacteria to secnidazole, metronidazole, tinidazole and clindamycin. A total of 605 unique BV-related bacteria and 108 isolates of lactobacilli recovered from the human vagina of US women during the years 2009-2015 were tested for antimicrobial susceptibility by the agar dilution CLSI reference method to determine the minimal inhibitory concentration (MIC)...
May 15, 2017: Anaerobe
https://www.readbyqxmd.com/read/28520511/upregulation-of-acref-in-quinolone-resistance-development-in-escherichia-coli-when-acrab-tolc-function-is-impaired
#16
Chuan-Zhen Zhang, Man-Xia Chang, Lei Yang, Yan-Yan Liu, Pin-Xian Chen, Hong-Xia Jiang
We studied mechanisms of drug resistance development in Escherichia coli strains lacking efflux pump components. E. coli K12 deletion mutants were subjected to increasing concentrations of ciprofloxacin (CIP) to determine the frequency of target gene mutations. We generated a series of mutants that were selected based on their minimum inhibitory concentrations (MICs) to CIP, as well as their corresponding point mutations in target genes. The mutants displayed a number of target modifications and, in particular, gyrA mutations altering codons Ser83Leu, Asp87Gly, and Asp87His as well as a change in parC at 78 (substitution of Gly for Asp)...
May 18, 2017: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/28516432/measurement-of-piperacillin-plasma-concentrations-in-cancer-patients-with-suspected-infection
#17
Tobias Rachow, Verena Schlüter, Sibylle Bremer-Streck, Udo Lindig, Sebastian Scholl, Peter Schlattmann, Michael Kiehntopf, Andreas Hochhaus, Marie von Lilienfeld-Toal
BACKGROUND: Piperacillin (PIP) in combination with tazobactam is commonly used for anti-infective treatment in cancer patients. PIP exerts a time-dependent killing. Thus, the maintenance of plasma concentrations above a pre-defined target concentration for a pre-defined time may be relevant for optimal efficacy. It is assumed that PIP-plasma concentrations above the clinical breakpoint of the target pathogen [Pseudomonas aeruginosa, clinical breakpoint at minimal inhibitory concentration (MIC) 16 mg/L] should be reached for 100% of the dosing interval or >4xMIC (64 mg/L) for 50% of the dosing interval...
May 17, 2017: Infection
https://www.readbyqxmd.com/read/28516003/mode-of-action-of-the-2-phenylquinoline-efflux-inhibitor-pqq4r-against-escherichia-coli
#18
Diana Machado, Laura Fernandes, Sofia S Costa, Rolando Cannalire, Giuseppe Manfroni, Oriana Tabarrini, Isabel Couto, Stefano Sabatini, Miguel Viveiros
Efflux pump inhibitors are of great interest since their use as adjuvants of bacterial chemotherapy can increase the intracellular concentrations of the antibiotics and assist in the battle against the rising of antibiotic-resistant bacteria. In this work, we have described the mode of action of the 2-phenylquinoline efflux inhibitor (4-(2-(piperazin-1-yl)ethoxy)-2-(4-propoxyphenyl) quinolone - PQQ4R), against Escherichia coli, by studding its efflux inhibitory ability, its synergistic activity in combination with antibiotics, and compared its effects with the inhibitors phenyl-arginine-β-naphthylamide (PAβN) and chlorpromazine (CPZ)...
2017: PeerJ
https://www.readbyqxmd.com/read/28513771/species-distribution-and-antifungal-susceptibility-patterns-of-candida-isolates-from-a-public-tertiary-teaching-hospital-in-the-eastern-cape-province-south-africa
#19
P Mnge, B I Okeleye, S D Vasaikar, T Apalata
Candida species are the leading cause of invasive fungal infections, and over the past decade there has been an increased isolation of drug resistant Candida species. This study aimed to identify the species distribution of Candida isolates and to determine their unique antifungal susceptibility and resistance patterns. During a cross-sectional study, 209 Candida isolates (recovered from 206 clinical samples) were collected and their species distribution was determined using ChromAgar Candida. The Vitek-2 system (Biomerieux, South Africa) was used to determine minimum inhibitory concentrations (MICs) to azoles (fluconazole, voriconazole), echinocandins (caspofungin, micafungin), polyenes (amphotericin B) and flucytosine...
May 15, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28510695/effects-of-an-autoinducer-analogue-on-antibiotic-tolerance-in-pseudomonas-aeruginosa
#20
Takashi Amoh, Keiji Murakami, Reiko Kariyama, Kenji Hori, Darija Viducic, Katsuhiko Hirota, Jun Igarashi, Hiroaki Suga, Matthew R Parsek, Hiromi Kumon, Yoichiro Miyake
Objectives: Antibiotic tolerance causes chronic, refractory and persistent infections. In order to advance the development of a new type of drug for the treatment of infectious diseases, we herein investigated the effects of a newly synthesized analogue of the Pseudomonas aeruginosa quorum-sensing autoinducer named AIA-1 ( a uto i nducer a nalogue) on antibiotic tolerance in P. aeruginosa . Methods: A P. aeruginosa luminescent strain derived from PAO1 was injected into neutropenic ICR mice and bioluminescence images were acquired for a period of time after treatments with antibiotics and AIA-1...
May 16, 2017: Journal of Antimicrobial Chemotherapy
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