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Nitroimidazoles

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https://www.readbyqxmd.com/read/28741367/radiotherapy-synergizes-with-the-hypoxia-activated-prodrug-evofosfamide-in-vitro-and-in-vivo-studies
#1
Yoichi Takakusagi, Shun Kishimoto, Naz Sarwat, Shingo Matsumoto, Keita Saito, Charles Hart, James B Mitchell, Murali K Cherukuri
AIMS: Evofosfamide (TH-302) is a hypoxia-activated prodrug (HAP) which releases the DNA damaging bromo-isophosphoramide (Br-IPM) moiety selectively under hypoxic conditions. Since solid tumors are known to have hypoxic regions, HAPs in combination with chemotherapy or radiotherapy will be beneficial. We tested the oxygen dependence of the release kinetics of Br-IPM using Electron Paramagnetic Resonance (EPR) with spin trapping by monitoring the redox-cycling the nitroimidazole moiety of TH-302 and oxygen dependence of TH-302 on in vitro cytotoxicity at different levels of hypoxia was also examined...
July 25, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28740613/synthesis-and-biological-evaluation-of-paclitaxel-and-camptothecin-prodrugs-on-the-basis-of-2-nitroimidazole
#2
Chen Jin, Shuai Wen, Qiumeng Zhang, Qiwen Zhu, Jiahui Yu, Wei Lu
Due to the low esterase activity in human plasma, many ester and carbonate prodrugs tested in humans may be less effective than that in preclinical animals. In this letter, PTX and SN-38 were attached to the N-1 position of 2-nitroimidazole via a carbonate linker. Presumably, 2-aminoimidazole may help promote the intramolecular hydrolysis of the carbonate bond. The prodrugs exhibited a considerable stability in buffers at different pH values as well as in human plasma. Furthermore, a rapid reduction was exhibited in the presence of nitroreductase...
July 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28738704/insights-into-the-binding-mode-of-sulphamates-and-sulphamides-to-hca-ii-crystallographic-studies-and-binding-free-energy-calculations
#3
Giuseppina De Simone, Emma Langella, Davide Esposito, Claudiu T Supuran, Simona Maria Monti, Jean-Yves Winum, Vincenzo Alterio
Sulphamate and sulphamide derivatives have been largely investigated as carbonic anhydrase inhibitors (CAIs) by means of different experimental techniques. However, the structural determinants responsible for their different binding mode to the enzyme active site were not clearly defined so far. In this paper, we report the X-ray crystal structure of hCA II in complex with a sulphamate inhibitor incorporating a nitroimidazole moiety. The comparison with the structure of hCA II in complex with its sulphamide analogue revealed that the two inhibitors adopt a completely different binding mode within the hCA II active site...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28715020/2-nitroimidazole-based-fluorescent-probes-for-nitroreductase-monitoring-reductive-stress-in-cellulo
#4
X Ao, S A Bright, N C Taylor, R B P Elmes
Two 2-nitroimidazole-1,8-naphthalimide conjugates, 1 and 2, have been synthesised as fluorescence probes for the detection of reductive stress in HeLa cells. The 4-substituted derivative 1 was shown to act as a highly sensitive and selective substrate for nitroreductase where it exhibited a clear blue to green ratiometric fluorescence response visible to the naked eye. Moreover, biological studies demonstrated 1 could be activated in cellulo where the impact of reductive stress was easily monitored using confocal microscopy and flow cytommetry...
July 17, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28707620/a-quechers-based-sample-preparation-method-for-the-analysis-of-5-nitroimidazoles-in-bovine-milk-by-hplc-dad
#5
Tomasz Tuzimski, Tomasz Rejczak
In this study, a simple, cost-effective, and sensitive HPLC diode-array detection method was developed for thesimultaneous determination of six different 5-nitroimidazoles [metronidazole, 2-hydroxymethyl-1-methyl-5-nitro-(1)H-imidazole, dimetridazole (DMZ), ronidazole, ornidazole, and ipronidazole] in bovine milk samples. A QuEChERS-based sample preparation procedure was optimized by evaluating different cleanup sorbents, including zirconium-based sorbents (Z-Sep and Z-Sep+), C18, and primary–secondary amine (PSA), as well as EMR-Lipid cleanup solution...
July 13, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28695572/isomer-selectivity-in-low-energy-electron-attachment-to-nitroimidazoles
#6
Anita Ribar, Katharina Fink, Michael Probst, Stefan E Huber, Linda Feketeová, Stephan Denifl
Low-energy electrons effectively decompose the isomers 2-nitroimidazole and 4(5)-nitroimidazole by dissociative electron attachment (DEA) into a variety of fragment anions and radicals. We show in the present study that a distinct selectivity in the DEA reactions for the two isomers occurs. Several new decay channels are observed for 2-nitroimidazole including a dominant one leading to the loss of molecular H2O via the attachment of a low-energy electron. In contrast, the loss of a single hydrogen atom is a much more efficient reaction in DEA to 4(5)-nitroimidazole...
July 11, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28659886/molecular-epidemiology-and-risk-factors-of-carbapenem-resistant-klebsiella-pneumoniae-infections-in-eastern-china
#7
Bing Zheng, Yingxin Dai, Yang Liu, Weiyang Shi, Erkuan Dai, Yichao Han, Dandan Zheng, Yuetian Yu, Min Li
Background: The increasing prevalence of carbapenem-resistant Klebsiella pneumoniae (CRKP) poses an immediate threat to treatment worldwide. This retrospective study assessed the molecular epidemiology and determined the risk factors for and outcomes of CRKP infections in a general teaching hospital in Shanghai, China. Methods: From January 2013 to July 2015, 100 consecutive unique CRKP isolates isolated from hospitalized patients were collected. Isolates were screened for antibiotic resistance genes by polymerase chain reaction and molecular typing was performed by pulsed-field gel electrophoresis (PFGE)...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28624613/nitroimidazole-refractory-giardiasis-a-growing-problem-requiring-rational-solutions
#8
REVIEW
E R Carter, L E Nabarro, L Hedley, P L Chiodini
BACKGROUND: Giardia intestinalis is microaerophillic diarrhoea-causing protozoan common in countries with suboptimal sanitation. Standard treatment is with nitroimidazoles but a growing number of refractory cases are being reported. Treatment failure has become increasingly prevalent in travellers who contract giardiasis in Asia. Clinicians are increasingly falling back on second line and less well known drugs to treat giardiasis. AIMS: To review nitroimidazole-refractory G...
June 14, 2017: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/28619503/clinical-pharmacokinetics-of-levornidazole-in-elderly-subjects-and-dosing-regimen-evaluation-using-pharmacokinetic-pharmacodynamic-analysis
#9
Beining Guo, Gaoli He, Xiaojie Wu, Jicheng Yu, Guoying Cao, Yi Li, Yaxin Fan, Yuancheng Chen, Yaoguo Shi, Yingyuan Zhang, Jing Zhang
PURPOSE: Levornidazole, the levo-isomer of ornidazole, is a third-generation nitroimidazole derivative newly developed after metronidazole, tinidazole, and ornidazole. An open-label, parallel-controlled, single-dose study was conducted for the investigation of the pharmacokinetic (PK) profile of levornidazole and its metabolites in healthy elderly Chinese subjects, and for the evaluation of 2 dosing regimens in the elderly. METHODS: Levornidazole was intravenously administered at 500 mg to healthy elderly (aged 60-80 years) or young subjects (aged 19-45 years)...
July 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28580362/kemtub012-ni2-a-novel-potent-tubulysin-analog-that-selectively-targets-hypoxic-cancer-cells-and-is-potentiated-by-cytochrome-p450-reductase-downregulation
#10
Paolo Lazzari, Marco Spiga, Monica Sani, Matteo Zanda, Ian N Fleming
PURPOSE: There is an urgent need to develop effective therapies and treatment strategies to treat hypoxic tumors, which have a very poor prognosis and do not respond well to existing therapies. METHODS: A novel hypoxia-targeting agent, KEMTUB012-NI2, was synthesized by conjugating a 2-nitroimidazole hypoxia-targeting moiety to a synthetic tubulysin, a very potent antimitotic. Its hypoxic selectivity and mode of action were studied in breast cancer cell lines. RESULTS: KEMTUB012-NI2 exhibited a similar selectivity for hypoxic cells to that of tirapazamine, a well-established hypoxia-targeting agent, but was >1,000 times more potent in cell cytotoxicity assays...
2017: Hypoxia
https://www.readbyqxmd.com/read/28552479/biopharmaceutic-parameters-pharmacokinetics-transport-and-cyp-mediated-drug-interactions-of-iiim-017-a-novel-nitroimidazooxazole-analogue-with-anti-tuberculosis-activity
#11
Gurleen Kour, Parvinder Pal Singh, Asha Bhagat, Zabeer Ahmed
Nitroimidazoles are emerging as a new class of therapeutic agents with potent anti-tubercular activity. CSIR-IIIM has synthesized a novel nitrohydroimidazooxazole (NHIO) analogue, IIIM-017 with a MIC of 0.37μg/ml (against H37Rv). Here, we aim at further exploration of physicochemical properties and preclinical absorption, metabolism, disposition and pharmacokinetics of IIIM-017. In this study, in silico physicochemical parameters, lipophilicity, permeability, transport, hepatotoxicity, CYP mediated drug interactions and pharmacokinetics of IIIM-017 were investigated...
August 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28551144/multiresidue-method-for-identification-and-quantification-of-avermectins-benzimidazoles-and-nitroimidazoles-residues-in-bovine-muscle-tissue-by-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry-uhplc-ms-ms-using-a-quechers-approach
#12
Guilherme Resende da Silva, Josefa Abucater Lima, Leonardo Francisco de Souza, Flávio Alves Santos, Mary Ane Gonçalves Lana, Débora Cristina Sampaio de Assis, Silvana de Vasconcelos Cançado
A quantitative and confirmatory multiresidue method for determining the presence of avermectins, benzimidazoles and nitroimidazoles in bovine muscle tissue by ultra-high performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) was developed, optimized and validated, using a QuEChERS extraction. The evaluated performance parameters were linearity, selectivity, matrix effect, decision limits (CCα), detection capability (CCβ), limits of detection (LOD), limits of quantification (LOQ), accuracy, precision and robustness...
August 15, 2017: Talanta
https://www.readbyqxmd.com/read/28535278/nimh-a-novel-nitroimidazole-resistance-gene-contributing-to-metronidazole-resistance-in-bacteroides-fragilis
#13
Corentine Alauzet, Sibel Berger, Hélène Jean-Pierre, Luc Dubreuil, Estelle Jumas-Bilak, Alain Lozniewski, Hélène Marchandin
No abstract text is available yet for this article.
May 23, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28522362/susceptibility-of-bacterial-vaginosis-bv-associated-bacteria-to-secnidazole-compared-to-metronidazole-tinidazole-and-clindamycin
#14
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/28503897/aggregate-formation-of-oligonucleotides-that-assisted-molecular-imaging-for-tracking-of-oxygen-status-in-tumor-tissue
#15
Kazuki Yoshihara, Kohei Takagi, Aoi Son, Ryohsuke Kurihara, Kazuhito Tanabe
The use of DNA aggregates could be a promising strategy for molecular imaging of biological functions. Herein, phosphorescent oligodeoxynucleotides were designed with the aim of visualizing oxygen fluctuation in tumor cells. We prepared DNA-ruthenium conjugate (DRCs) that consisted of oligodeoxynucleotides, a phosphorescent ruthenium complex, a pyrene unit for high oxygen responsiveness, and a nitroimidazole unit as a tumor-targeting unit. In general, oligonucleotides have low cell permeability because of their own negative charges; however, the present DRC formed aggregates in aqueous solution due to the hydrophobic pyrene and nitroimidazole groups, and smoothly penetrated the cellular membrane to accumulate in tumor cells in a hypoxia-selective manner...
May 14, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28494608/parenteral-nutrition-in-childhood-and-consequences-for-dentition-and-gingivae
#16
D Olczak-Kowalczyk, M Danko, E Banaś, D Gozdowski, K Popińska, E Krasuska-Sławińska, J Książyk
AIM: Assessment of dentition in children under parenteral nutrition, risk factors for caries, and dental developmental abnormalities. MATERIALS AND METHODS: The study involved 63 patients (aged 2.25-16.6 years), i.e. 32 subjects receiving parenteral nutrition for a mean period of 5.6±2.94 years, and 31 healthy control subjects. Oral hygiene (OHI-S, PL-I), gingival (GI), and dentition status (caries, DMFT/dmft, enamel defects, shape alterations), frequency of oral meals and frequency of cariogenic snacks consumption were evaluated...
March 2017: European Journal of Paediatric Dentistry: Official Journal of European Academy of Paediatric Dentistry
https://www.readbyqxmd.com/read/28463485/nitroimidazoles-molecular-fireworks-that-combat-a-broad-spectrum-of-infectious-diseases
#17
Chee Wei Ang, Angie M Jarrad, Matthew A Cooper, Mark A T Blaskovich
Infectious diseases claim millions of lives every year, but with the advent of drug resistance, therapeutic options to treat infections are inadequate. There is now an urgent need to develop new and effective treatments. Nitroimidazoles are a class of antimicrobial drugs that have remarkable broad spectrum activity against parasites, mycobacteria, and anaerobic Gram-positive and Gram-negative bacteria. While nitroimidazoles were discovered in the 1950s, there has been renewed interest in their therapeutic potential, particularly for the treatment of parasitic infections and tuberculosis...
May 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28462832/6-nitro-2-3-dihydroimidazo-2-1-b-1-3-thiazoles-facile-synthesis-and-comparative-appraisal-against-tuberculosis-and-neglected-tropical-diseases
#18
Andrew M Thompson, Adrian Blaser, Brian D Palmer, Robert F Anderson, Sujata S Shinde, Delphine Launay, Eric Chatelain, Louis Maes, Scott G Franzblau, Baojie Wan, Yuehong Wang, Zhenkun Ma, William A Denny
As part of a quest for backups to the antitubercular drug pretomanid (PA-824), we investigated the unexplored 6-nitro-2,3-dihydroimidazo[2,1-b][1,3]-thiazoles and related -oxazoles. The nitroimidazothiazoles were prepared in high yield from 2-bromo-4-nitroimidazole via heating with substituted thiiranes and diisopropylethylamine. Equivalent examples of these two structural classes provided broadly comparable MICs, with 2-methyl substitution and extended aryloxymethyl side chains preferred; albeit, S-oxidised thiazoles were ineffective for tuberculosis...
March 27, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28456516/identification-of-novel-1-indolyl-acetate-5-nitroimidazole-derivatives-of-combretastatin-a-4-as-potential-tubulin-polymerization-inhibitors
#19
Yong-Fang Yao, Zhong-Chang Wang, Song-Yu Wu, Qing-Fang Li, Chen Yu, Xin-Yi Liang, Peng-Cheng Lv, Yong-Tao Duan, Hai-Liang Zhu
Microtubules are essential for the mitotic division of cells and have become an attractive target for anti-tumour drugs due to the increased incidence of cancer and significant mitosis rate of tumour cells. In this study, a total of six indole 1-position modified 1-indolyl acetate-5-nitroimidazole derivatives were designed, synthesized, and evaluated for their ability to inhibit tubulin polymerization caused by binding to the colchicine-binding site of tubulin. Among them, compound 3 displayed the best ability to inhibit tubulin polymerization; it also exhibited better anti-proliferative activities than colchicine against a panel of human cancer cells (with IC50 values ranging from 15 to 40nM), especially HeLa cells (with IC50 values of 15nM), based on the cellular cytotoxicity assay results...
August 1, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28453841/the-use-of-quinacrine-in-nitroimidazole-resistant-giardia-duodenalis-an-old-drug-for-an-emerging-problem
#20
MULTICENTER STUDY
Ana Requena-Méndez, Pilar Goñi, Encarnación Rubio, Diana Pou, Victoria Fumadó, Silvia Lóbez, Edelweiss Aldasoro, Juan Cabezos, Maria Eugenia Valls, Begoña Treviño, Antonio Federico Martínez Montseny, Antonio Clavel, Joaquim Gascon, José Muñoz
Background.: There is little evidence regarding the management of refractory giardiasis after treatment with nitroimidazoles. This study estimates the proportion of persistent giardiasis in 3 hospitals in Barcelona, describes associated risk factors and genotype, and evaluates the efficacy rate of quinacrine in those with persistent giardiasis. Methods.: A clinical, prospective, observational study was conducted in patients with giardiasis treated with nitroimidazoles...
March 15, 2017: Journal of Infectious Diseases
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