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Nitroimidazoles

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https://www.readbyqxmd.com/read/28624613/nitroimidazole-refractory-giardiasis-a-growing-problem-requiring-rational-solutions
#1
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
#2
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)...
June 12, 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
#3
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
#4
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...
May 26, 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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
https://www.readbyqxmd.com/read/28436019/antibiotic-therapy-for-pelvic-inflammatory-disease
#14
REVIEW
Ricardo F Savaris, Daniele G Fuhrich, Rui V Duarte, Sebastian Franik, Jonathan Ross
BACKGROUND: Pelvic inflammatory disease (PID) is an infection that affects 4% to 12% of young women, and is one of the most common causes of morbidity in this age group. The main intervention for acute PID is the use of broad-spectrum antibiotics which cover Chlamydia trachomatis, Neisseria gonorrhoeae, and anaerobic bacteria, administered intravenously, intramuscularly, or orally. In this review, we assessed the optimal treatment regimen for PID. OBJECTIVES: To assess the effectiveness and safety of antibiotic regimens used to treat pelvic inflammatory disease...
April 24, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28414944/direct-and-indirect-electrochemical-reduction-prior-to-a-biological-treatment-for-dimetridazole-removal
#15
Melika Zaghdoudi, Florence Fourcade, Isabelle Soutrel, Didier Floner, Abdeltif Amrane, Hager Maghraoui-Meherzi, Florence Geneste
Two different electrochemical reduction processes for the removal of dimetridazole, a nitroimidazole-based antibiotic, were examined in this work. A direct electrochemical reduction was first carried out in a home-made flow cell in acidic medium at potentials chosen to minimize the formation of amino derivatives and then the formation of azo dimer. Analysis of the electrolyzed solution showed a total degradation of dimetridazole and the BOD5/COD ratio increased from 0.13 to 0.24. An indirect electrochemical reduction in the presence of titanocene dichloride ((C5H5)2TiCl2), which is used to reduce selectively nitro compounds, was then investigated to favour the formation of amino compounds over hydroxylamines and then to prevent the formation of azo and azoxy dimers...
April 9, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28396548/click-chemistry-facilitated-structural-diversification-of-nitrothiazoles-nitrofurans-and-nitropyrroles-enhances-antimicrobial-activity-against-giardia-lamblia
#16
Wan Jung Kim, Keith A Korthals, Suhua Li, Christine Le, Jarosław Kalisiak, K Barry Sharpless, Valery V Fokin, Yukiko Miyamoto, Lars Eckmann
Giardia lamblia is an important and ubiquitous cause of diarrheal disease. The primary agents in the treatment of giardiasis are nitroheterocyclic drugs, particularly the imidazoles metronidazole and tinidazole and the thiazole nitazoxanide. Although these drugs are generally effective, treatment failures occur in up to 20% of cases, and resistance has been demonstrated in vivo and in vitro Prior work had suggested that side chain modifications of the imidazole core can lead to new effective 5-nitroimidazole drugs that can combat nitro drug resistance, but the full potential of nitroheterocycles other than imidazole to yield effective new antigiardial agents has not been explored...
June 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28332260/biological-characterization-of-novel-nitroimidazole-peptide-conjugates-in-vitro-and-in-vivo
#17
Ralf Bergmann, Katrin Splith, Jens Pietzsch, Michael Bachmann, Ines Neundorf
Recently, we reported on the design of a multimodal peptide conjugate useful as delivery platform for targeting hypoxic cells. A nitroimidazole (2-(2-nitroimidazol-1-yl)acetic acid, NIA) moiety, which is selectively entrapped in hypoxic cells, was coupled to a cell-penetrating peptide serving as the transporter. Furthermore, attachment of a bifunctional linker allowed the introduction of a diagnostic or therapeutic radiometal. However, although selective tumor accumulation could be detected in vivo, a fast renal clearance of the compound was observed...
March 23, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28314825/increased-plasma-exposures-of-conjugated-metabolites-of-morinidazole-in-renal-failure-patients-a-critical-role-of-uremic-toxins
#18
Fandi Kong, Xiaoyan Pang, Kan Zhong, Zitao Guo, Xiuli Li, Dafang Zhong, Xiaoyan Chen
Morinidazole is a 5-nitroimidazole drug. Its sulfate conjugate M7 was a sensitive substrate of organic anion transporter 1 (OAT1) and OAT3, whereas N+-glucuronides M8-1 and M8-2 were only OAT3 substrates. In chronic renal failure (CRF) patients, plasma exposures of the three conjugates increased by 15-fold, which were also found in 5/6 nephrectomized (5/6 Nx) rats in this study. Although the transcriptions of Oat1 and Oat3 in 5/6 Nx rat kidneys decreased by 50%, no difference was observed on the three conjugate uptakes between control and 5/6 Nx rat kidney slices...
March 17, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28294075/%C3%AE-18f-fluoro-azomycin-arabinoside-%C3%AE-18f-faza-synthesis-radiofluorination-and-preliminary-pet-imaging-of-murine-a431-tumors
#19
Piyush Kumar, Peter Roselt, Gerald Reischl, Carlene Cullinane, Davood Beiki, Walter Ehrlichmann, David Binns, Ebrahim Naimi, Jennifer Yang, Rodney Hicks, Hans-Juergen Machulla, Leonard I Wiebe
BACKGROUND: 1-α-D-(5-Deoxy-5-[18F]fluoroarabinofuranosyl)-2-nitroimidazole ([18F]FAZA) is a PET radiotracer that demonstrates excellent potential in imaging regional hypoxia, and is clinically used in diagnosing a wide range of solid tumors in cancer patients. [18F]FAZA, however, is radiofluorinated in only moderate recovered radiochemical yield (rRCY, ~12%). It is postulated that the relative stability of the C1' β-anomeric bond at C5' will make 1-β-D-(5-fluoro-5-deoxyarabinofuranosyl)-2-nitroimidazole (β-FAZA), the β-conformer of FAZA, an attractive candidate for clinical hypoxia imaging...
March 13, 2017: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28243064/conjugation-of-metronidazole-with-dextran-a-potential-pharmaceutical-strategy-to-control-colonic-distribution-of-the-anti-amebic-drug-susceptible-to-metabolism-by-colonic-microbes
#20
Wooseong Kim, Yejin Yang, Dohoon Kim, Seongkeun Jeong, Jin-Wook Yoo, Jeong-Hyun Yoon, Yunjin Jung
Metronidazole (MTDZ), the drug of choice for the treatment of protozoal infections such as luminal amebiasis, is highly susceptible to colonic metabolism, which may hinder its conversion from a colon-specific prodrug to an effective anti-amebic agent targeting the entire large intestine. Thus, in an attempt to control the colonic distribution of the drug, a polymeric colon-specific prodrug, MTDZ conjugated to dextran via a succinate linker (Dex-SA-MTDZ), was designed. Upon treatment with dextranase for 8 h, the degree of Dex-SA-MTDZ depolymerization (%) with a degree of substitution (mg of MTDZ bound in 100 mg of Dex-SA-MTDZ) of 7, 17, and 30 was 72, 38, and 8, respectively, while that of dextran was 85...
2017: Drug Design, Development and Therapy
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