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Sara Ranjbar, Najmeh Edraki, Mahsima Khoshneviszadeh, Alireza Foroumadi, Ramin Miri, Mehdi Khoshneviszadeh
Mammalian target of rapamycin (mTOR) is a phosphoinositide 3-kinase-related protein kinase which controls cell growth and is frequently deregulated in many cancers. Therefore, mTOR inhibitors are used as antineoplastic agents for cancer treatment. In this study, 1,2,4-triazine derivatives containing different arylidene-hydrazinyl moieties were designed and synthesized. Cytotoxicity of the compounds was evaluated on HL-60 and MCF-7 cell lines by MTT assay. S1, S2 and S3 exhibited good cytotoxic activity on both cell lines with an IC50 range of 6...
February 2018: Research in Pharmaceutical Sciences
Atmika Paudel, Suresh Panthee, Makoto Urai, Hiroshi Hamamoto, Tomohiko Ohwada, Kazuhisa Sekimizu
Poor pharmacokinetic parameters are a major reason for the lack of therapeutic activity of some drug candidates. Determining the pharmacokinetic parameters of drug candidates at an early stage of development requires an inexpensive animal model with few associated ethical issues. In this study, we used the silkworm infection model to perform structure-activity relationship studies of an antimicrobial agent, GPI0039, a novel nitrofuran dichloro-benzyl ester, and successfully identified compound 5, a nitrothiophene dichloro-benzyl ester, as a potent antimicrobial agent with superior therapeutic activity in the silkworm infection model...
January 25, 2018: Scientific Reports
A J Stewardson, J Vervoort, N Adriaenssens, S Coenen, M Godycki-Cwirko, A Kowalczyk, B D Huttner, C Lammens, S Malhotra-Kumar, H Goossens, S Harbarth
OBJECTIVES: We quantified the impact of antibiotics prescribed in primary care for urinary tract infections (UTIs) on intestinal colonization by ciprofloxacin-resistant (CIP-RE) and extended-spectrum β-lactamase-producing Enterobacteriaceae (ESBL-PE), while accounting for household clustering. METHODS: Prospective cohort study from January 2011 to August 2013 at primary care sites in Belgium, Poland and Switzerland. We recruited outpatients requiring antibiotics for suspected UTIs or asymptomatic bacteriuria (exposed patients), outpatients not requiring antibiotics (non-exposed patients), and one to three household contacts for each patient...
January 10, 2018: Clinical Microbiology and Infection
Fadi Aldeek, Kevin Hsieh, Obiadada Ugochukwu, Ghislain Gerard, Walter Hammack
We developed and validated a method for the extraction, identification, and quantitation of four nitrofuran metabolites: (3-amino-2-oxazolidinone (AOZ); 3-amino-5-morpholinomethyl-2-oxazolidinone (AMOZ); semicarbazide (SC); and 1-aminohydantoin (AHD)), as well as chloramphenicol and florfenicol, in a variety of seafood commodities. Samples were extracted by liquid-liquid extraction techniques, analyzed by UHPLC-MS/MS, and quantitated using commercially sourced, derivatized nitrofuran metabolites, with their isotopically-labelled internal standards in-solvent...
December 28, 2017: Journal of Agricultural and Food Chemistry
Fanny Palace-Berl, Kerly Fernanda Mesquita Pasqualoto, Bianca Zingales, Carolina Borsoi Moraes, Mariana Bury, Caio Haddad Franco, Adelson Lopes da Silva Neto, João Sussumu Murayama, Solange Lessa Nunes, Marcelo Nunes Silva, Leoberto Costa Tavares
Chagas disease, caused by the protozoan Trypanosoma cruzi, is a neglected chronic tropical infection endemic in Latin America. New and effective treatments are urgently needed because the two available drugs - benznidazole (BZD) and nifurtimox (NFX) - have limited curative power in the chronic phase of the disease. We have previously reported the design and synthesis of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides that showed high trypanocidal activity against axenic epimastigote forms of three T...
December 5, 2017: European Journal of Medicinal Chemistry
Alireza Foroumadi, Hadi Adibi, Sussan Kabudanian Ardestani, Samira Shirooie, Arezoo Bozorgomid, Ali Jafari
A series of ( 5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a-6e have been synthesized and screened for in-vitro anti-leishmanial activity against the promastigote form of L. major . The structure of Schiff bases were confirmed by1 H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes of L. major in comparison toglucantime (IC50 3× 103 μg/mL). Meta and Para substitutions in benzene ring containing compounds were more potent than other derivative and the most potent compounds were 6d, 6e with IC50 value 94 µm and 77...
2017: Iranian Journal of Pharmaceutical Research: IJPR
Brian T Veach, Renea Anglin, Thilak K Mudalige, Paula J Barnes
This paper describes a rapid and robust method utilizing a single liquid–liquid extraction for the quantitation and confirmation of chloramphenicol, florfenicol, and nitrofuran metabolites in honey. This methodology combines two previous extraction methods into a single extraction procedure and utilizes matrix-matched calibration standards and stable isotopically labeled standards to improve quantitation. The combined extraction procedure reduces the average extraction time by >50% when compared with previously used procedures...
November 30, 2017: Journal of AOAC International
Azar Tahghighi, Alireza Foroumadi, Susan Kabudanian-Ardestani, Seyed Mohammad Amin Mahdian
BACKGROUND: Cutaneous Leishmaniasis (CL) is endemic in many tropical and subtropical regions of the world. Due to the prolonged duration of therapy, adverse effect and resistance to current drugs in the treatment of CL, the discovery of novel, efficient, and safe leishmanicidal drugs is required. The aims of the present study was to synthesis of new compounds based on the active compounds of 5-(5-nitrofuran-2-yl)- and 5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazole bearing the linear amino alcohol of 3-aminopropan-1-ol in the C-2 position of thiadiazole ring and evaluation of their activity against the promastigote and amastigote forms of Leishmania major...
March 2017: Journal of Arthropod-borne Diseases
Elham Jafari, Tahereh Mohammadi, Ali Jahanian-Najafabadi, Farshid Hassanzadeh
1,3,4-oxadiazoles are interesting compounds because of their valuable biological effects such as cytotoxic, antibacterial, antifungal, and anti-tubercular activities. Ethyl mandelate was treated with hydrazine hydrate to yield the corresponding acylhydrazide. Some of the 2,5 disubstituted 1,3,4-oxadiazole derivatives were prepared from acylhydrazide using three different procedures. In the first procedure, acylhydrazide was reacted with nitro or chloro aroyle chloride to afford a diacylhydrazide which was cyclized to 2,5-disubstituted 1,3,4-oxadiazole in the presence of phosphoryl chloride as dehydrating agent...
August 2017: Research in Pharmaceutical Sciences
(no author information available yet)
The evidence regarding an association between the nitrofuran and sulfonamide classes of antibiotics and birth defects is mixed. As with all patients, antibiotics should be prescribed for pregnant women only for appropriate indications and for the shortest effective duration. During the second and third trimesters, sulfonamides and nitrofurantoins may continue to be used as first-line agents for the treatment and prevention of urinary tract infections and other infections caused by susceptible organisms. Prescribing sulfonamides or nitrofurantoin in the first trimester is still considered appropriate when no other suitable alternative antibiotics are available...
September 2017: Obstetrics and Gynecology
(no author information available yet)
The evidence regarding an association between the nitrofuran and sulfonamide classes of antibiotics and birth defects is mixed. As with all patients, antibiotics should be prescribed for pregnant women only for appropriate indications and for the shortest effective duration. During the second and third trimesters, sulfonamides and nitrofurantoins may continue to be used as first-line agents for the treatment and prevention of urinary tract infections and other infections caused by susceptible organisms. Prescribing sulfonamides or nitrofurantoin in the first trimester is still considered appropriate when no other suitable alternative antibiotics are available...
September 2017: Obstetrics and Gynecology
Feng Zhang, Hua Yao, Yifan Zhao, Xing Li, Gaowei Zhang, Yangyi Yang
The detection of antibiotics is critical and challenging due to the pervasive use of antibiotics had inevitably brought some negative impacts on ecosystem and human health. Herein, we reported an anti-interfere ability enhanced luminescent sensor of lanthanide metal-organic framework (Ln-MOF) filled mixed matrix membranes (MMMs), which combining the processibility of poly(methyl methacrylate) (PMMA) polymer with Ln-MOF of {[Tb2(AIP)2(H2O)10]·(AIP)·4H2O}n (Tb-AIP, where AIP is 5-aminoisophthalate) fillers...
November 1, 2017: Talanta
Karen P H Mattos, Marília B Visacri, Júlia C F Quintanilha, Gustavo R Lloret, Maria A Cursino, Anna S Levin, Carlos E Levy, Patricia Moriel
OBJECTIVE: The aim of this study was to determine the impact of two resolutions to restrict antibiotic use (RDCs no. 44/2010 and 20/2011) in the Campinas metropolitan area (Sao Paulo, Brazil) on antibiotic consumption, resistance rates, and trends in Escherichia coli-causing community-acquired urinary tract infection (UTI). METHODS: The annual retail sale information of antibiotics from drugstores in the Campinas metropolitan area between 2008 and 2012 were obtained through the Intercontinental Medical Statistics Health of Brazil...
September 2017: Journal of Global Antimicrobial Resistance
Deyong Kong, Hui Yun, Dan Cui, Mengyuan Qi, Chunyan Shao, Dichen Cui, Nanqi Ren, Bin Liang, Aijie Wang
Bioelectrodegradation of various organic pollutants has been extensively studied. However, whether different cathode potentials could alter the antimicrobial-degrading biocathode community structure and composition remain poorly understood. Here, the microbial community structure and composition of the nitrofurans nitrofurazone (NFZ) degrading biocathode in response to different cathode potentials (-0.45±0.01, -0.65±0.01 and -0.86±0.05V vs standard hydrogen electrode, with applied cell voltages of 0.2, 0...
October 2017: Bioresource Technology
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...
August 1, 2017: Bioorganic & Medicinal Chemistry
Kun Wang, Kunde Lin, Xinwen Huang, Meng Chen
The purpose of this study was to develop and validate a simple, fast, and specific extraction method for the analysis of 64 antibiotics from nine classes (including sulfonamides, quinolones, tetracyclines, macrolides, lincosamide, nitrofurans, β-lactams, nitromidazoles, and cloramphenicols) in chicken eggs. Briefly, egg samples were simply extracted with a mixture of acetonitrile-water (90:10, v/v) and 0.1 mol·L(-1) Na2EDTA solution assisted with ultrasonic. The extract was centrifuged, condensed, and directly analyzed on a liquid chromatography coupled to tandem mass spectrometry...
June 21, 2017: Journal of Agricultural and Food Chemistry
Thomas Y Cowie, Marcos Veguillas, Robert L Rae, Mathilde Rougé, Justyna M Żurek, Andrew W Prentice, Martin J Paterson, Magnus W P Bebbington
Nitrofurans undergo intramolecular Diels-Alder reactions with tethered electron-poor dienophiles more rapidly and in higher yield than non-nitrated furans. Computational studies indicate that increased stabilization of a partial positive charge on the nitro-substituted carbon in both transition state and product is the driving force for these reactions. Frontier molecular orbital energy differences indicate a switch from normal to inverse electron demand upon nitration. There does not appear to be a contribution from any differences in aromatic stabilization energy between furans and nitrofurans...
June 20, 2017: Journal of Organic Chemistry
Valérie Chalansonnet, Claire Mercier, Sylvain Orenga, Christophe Gilbert
BACKGROUND: Nitroreductases, NAD(P)H dependent flavoenzymes, are found in most of bacterial species. Even if Enterococcus faecalis strains seems to present such activity because of their sensitivity to nitrofurans, no enzyme has been described. Nitroreductases were separated of others reductases due to their capacity to reduce nitro compounds. They are further classified based on their preference in cofactor: NADH and/or NADPH. However, recently, azoreductases have been studied for their strong activity on nitro compounds, especially nitro pro-drugs...
May 25, 2017: BMC Microbiology
T Yu Vladimirova, L A Barishevskaya, A V Lyamin, O V Kondratenko, A K Velikanov
The purpose of the present study was to evaluate the effectiveness of nitrofuranes applied for the treatment of chronic tonsillitis. A total of 92 subjects divided into three cohorts were involved in this study. Cohort 1 included 43 patients presenting with decompensated chronic tonsillitis and having pathogens in palatine tonsil lacunae. Cohort 2 was comprised of 13 patients with compensated chronic tonsillitis having pathogenic microflora of the same localization, while Cohort 3 was composed of 36 patients resembling those of cohort 1 in terms of clinical presentation, pathogen composition, and microbial spectrum...
2017: Vestnik Otorinolaringologii
Egor V Verbitskiy, Svetlana A Baskakova, Natal'ya A Gerasimova, Natal'ya P Evstigneeva, Natal'ya V Zil'berberg, Nikolay V Kungurov, Marionella A Kravchenko, Sergey N Skornyakov, Marina G Pervova, Gennady L Rusinov, Oleg N Chupakhin, Valery N Charushin
A facile two-step synthetic approach to fluorinated and non-fluorinated 5-aryl-4-(5-nitrofuran-2-yl)-pyrimidines from readily available 5-bromo-4-(furan-2-yl)pyrimidine has been developed. All synthesized compounds were screened in vitro for their antibacterial activities against twelve various bacterial strains. It is demonstrated that some of these compounds exhibited significant antibacterial activities against strains Neisseria gonorrhoeae and Staphylococcus aureus, comparable and even higher with that commercial drug Spectinomycin...
July 1, 2017: Bioorganic & Medicinal Chemistry Letters
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