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Nitroimidazoles

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https://www.readbyqxmd.com/read/28436019/antibiotic-therapy-for-pelvic-inflammatory-disease
#1
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
#2
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
#3
Wan Jung Kim, Keith Korthals, Suhua Li, Christine Le, Jaroslaw 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 effective new 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...
April 10, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28332260/biological-characterization-of-novel-nitroimidazole-peptide-conjugates-in-vitro-and-in-vivo
#4
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
#5
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
#6
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
#7
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
https://www.readbyqxmd.com/read/28223799/hypoxia-responsive-ionizable-liposome-delivery-sirna-for-glioma-therapy
#8
Hong-Mei Liu, Ya-Fei Zhang, Yan-Dong Xie, Yi-Fan Cai, Bai-Yang Li, Wen Li, Ling-Yu Zeng, Yu-Ling Li, Ru-Tong Yu
Here, we report the hypoxia-responsive ionizable liposomes to deliver small interference RNA (siRNA) anticancer drugs, which can selectively enhance cellular uptake of the siRNA under hypoxic and low-pH conditions to cure glioma. For this purpose, malate dehydrogenase lipid molecules were synthesized, which contain nitroimidazole groups that impart hypoxia sensitivity and specificity as hydrophobic tails, and tertiary amines as hydrophilic head groups. These malate dehydrogenase molecules, together with DSPE-PEG2000 and cholesterol, were self-assembled into O'(1),O(1)-(3-(dimethylamino)propane-1,2-diyl) 16-bis(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl) di(hexadecanedioate) liposomes (MLP) to encapsulate siRNA through electrostatic interaction...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28213209/molecularly-imprinted-solid-phase-extraction-method-for-simultaneous-determination-of-seven-nitroimidazoles-from-honey-by-hplc-ms-ms
#9
Xiu-Chun Guo, Zhao-Yang Xia, Hai-Hui Wang, Wen-Yi Kang, Li-Ming Lin, Wen-Qing Cao, Hong-Wei Zhang, Wen-Hui Zhou
In this work, a selective sample cleanup procedure that combined molecular imprinting technique with solid phase extraction was developed for the simultaneous extraction of the seven nitroimidazoles (NMZs) from honey samples. The molecular imprinting polymers for NMZs were prepared through bulk polymerization method using 2-methyl-5-nitroimidazole as template molecule, methacrylic acid as the functional monomer and ethylene glycol dimethacrylate as the cross linking agent. The obtained molecular imprinting polymers showed high affinity to template molecule and was used as selective sorbent for simultaneously selective extraction of the seven NMZs from honey matrix...
May 1, 2017: Talanta
https://www.readbyqxmd.com/read/28180110/assessing-tumor-oxygenation-for-predicting-outcome-in-radiation-oncology-a-review-of-studies-correlating-tumor-hypoxic-status-and-outcome-in-the-preclinical-and-clinical-settings
#10
REVIEW
Florence Colliez, Bernard Gallez, Bénédicte F Jordan
Tumor hypoxia is recognized as a limiting factor for the efficacy of radiotherapy, because it enhances tumor radioresistance. It is strongly suggested that assessing tumor oxygenation could help to predict the outcome of cancer patients undergoing radiation therapy. Strategies have also been developed to alleviate tumor hypoxia in order to radiosensitize tumors. In addition, oxygen mapping is critically needed for intensity modulated radiation therapy (IMRT), in which the most hypoxic regions require higher radiation doses and the most oxygenated regions require lower radiation doses...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28178618/medicinal-plants-and-their-isolated-compounds-showing-anti-trichomonas-vaginalis-activity
#11
REVIEW
Mozhgan Mehriardestani, Atousa Aliahmadi, Tayebeh Toliat, Roja Rahimi
Trichomonas vaginalis is a major of non-viral sexually-transmitted infection and an important cause of serious obstetrical and gynecological complications. Treatment options for trichomoniasis are limited to nitroimidazole compounds. The increasing resistance and allergic reactions to nitroimidazole and recurrent trichomoniasis make it essential to identify and develop new drugs against trichomoniasis. Medicinal plants are an important source for discovery of new medications. This review discusses the anti-trichomonas effects of medicinal plants and their chemical constituents to find better options against this pathogenic protozoon...
April 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28164233/the-use-of-quinacrine-in-nitroimidazole-resistant-giardia-duodenalis-an-old-drug-for-an-emerging-problem
#12
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
No abstract text is available yet for this article.
February 6, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28151652/kinetic-study-of-hydroxyl-and-sulfate-radical-mediated-oxidation-of-pharmaceuticals-in-wastewater-effluents
#13
Lushi Lian, Bo Yao, Shaodong Hou, Jingyun Fang, Shuwen Yan, Weihua Song
Advanced oxidation processes (AOPs), such as hydroxyl radical (HO(•))- and sulfate radical (SO4(•-))-mediated oxidation, are alternatives for the attenuation of pharmaceuticals and personal care products (PPCPs) in wastewater effluents. However, the kinetics of these reactions needs to be investigated. In this study, kinetic models for 15 PPCPs were built to predict the degradation of PPCPs in both HO(•)- and SO4(•-)-mediated oxidation. In the UV/H2O2 process, a simplified kinetic model involving only steady state concentrations of HO(•) and its biomolecular reaction rate constants is suitable for predicting the removal of PPCPs, indicating the dominant role of HO(•) in the removal of PPCPs...
February 13, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28137470/nitroimidazole-derivatives-of-polypyridyl-ruthenium-complexes-towards-understanding-their-anticancer-activity-and-mode-of-action
#14
Olga Mazuryk, Oksana Krysiak-Foria, Agnieszka Żak, Franck Suzenet, Agata Ptak-Belowska, Tomasz Brzozowski, Grażyna Stochel, Małgorzata Brindell
The mechanism of cell death induced by the ruthenium polypyridyl complexes comprising two 4,7-diphenyl-1,10-phenanthroline ligands as well as one unmodified 2,2'-bipyridyl or modified with 2-nitroimidazole moiety attached by shorter (C3H6) or longer (C6H12) linker was investigated. Cytotoxicity and proliferation assays revealed that the studied Ru polypyridyl complexes are more toxic against human pancreas carcinoma PANC-1 cell line than normal human keratinocytes HaCaT with IC50 of 3-5μM. The Ru complexes despite accumulation in mitochondria do not lead to mitochondrial disfunction, though decreasing of mitochondrial Ca(2+) causes mitochondria membrane hyperpolarization...
April 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28127094/efficient-preparation-of-2-nitroimidazole-nucleosides-as-precursors-for-hypoxia-pet-tracers
#15
Petra Križková, Anna Wieczorek, Friedrich Hammerschmidt
ABSTRACT: 2-Deoxy-D-ribose was converted to α/β-mixtures of methyl 3-O-acetyl- and methyl 3-O-benzoyl-2-deoxy-5-(p-toluenesulfonyl)-D-ribofuranosides. These were reacted with boron trichloride to generate ribofuranosyl chlorides, which afforded precursors for tracers to image tumor hypoxia on substitution with salts of 2-nitroimidazole. The anomeric ratio of the nucleosides was delicately influenced by the reaction conditions. GRAPHICAL ABSTRACT: HASH(0x476ff18) ...
2017: Monatshefte Für Chemie
https://www.readbyqxmd.com/read/28110684/hydrothermal-synthesis-of-polyethylenimine-protected-high-luminescent-pt-nanoclusters-and-their-application-to-the-detection-of-nitroimidazoles
#16
Na Xu, Hong-Wei Li, Yuqing Wu
A novel one-step hydrothermal synthesis of highly fluorescent platinum nanoclusters protected by polyethylenimine (Pt-NCs@PEI) is described. The products are characterized well by UV-vis absorption, fluorescence spectra, X-ray photoelectron spectroscopy (XPS) and transmission electron microscopy (TEM) imaging. The Pt-NCs@PEI possess high quantum yield at 28%, which is the relatively high one among the reported Pt-NCs; especially, the synthesis is in one-step and the reaction time is much shorter (<1 h) than the related methods...
March 15, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28088075/development-of-a-hypoxia-triggered-and-hypoxic-radiosensitized-liposome-as-a-doxorubicin-carrier-to-promote-synergetic-chemo-radio-therapy-for-glioma
#17
Hongmei Liu, Yandong Xie, Yafei Zhang, Yifan Cai, Baiyang Li, Honglin Mao, Yingguo Liu, Jun Lu, Longzhen Zhang, Rutong Yu
The treatment of malignant primary brain tumors is challenging. Concomitant radiochemotherapy has become the standard clinical treatment for malignant glioma, but there are two critical challenges to overcome in order to increase efficacy. First, glioma is known to have increased resistant to radiation due to its intra-tumoral hypoxia. In addition, the blood-brain barrier (BBB) restricts the distribution of the chemotherapeutic agent to the brain. Therefore, we developed a hypoxic radiosensitizer-prodrug liposome (MLP), in order to deliver DOX to the tumor and to overcome the above challenges, achieving a synergistic chemo-/radiotherapy treatment of malignant glioma...
March 2017: Biomaterials
https://www.readbyqxmd.com/read/28054455/development-and-validation-of-a-liquid-chromatography-with-tandem-mass-spectrometry-method-for-the-determination-of-nitroimidazole-residues-in-beeswax
#18
Kamila Mitrowska, Maja Antczak
In this study, a new method for the determination of 12 nitroimidazoles and their hydroxymetabolites (metronidazole, hydroxymetronidazole, dimetridazole, ronidazole, hydroxydimetridazole, ipronidazole, hydroxyipronidazole, carnidazole, ornidazole, secnidazole, ternidazole, tinidazole) in beeswax has been developed and validated. The optimized sample preparation procedure included melting and dilution of beeswax in a mixture of n-hexane and isopropanol followed by extraction with 2% acetic acid. The extracts were purified on strong cation exchange based solid-phase extraction cartridges and evaporated in a vacuum system with vortex motion...
January 5, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28043690/covalent-triazine-framework-1-as-adsorbent-for-inline-solid-phase-extraction-high-performance-liquid-chromatographic-analysis-of-trace-nitroimidazoles-in-porcine-liver-and-environmental-waters
#19
Cheng Zhong, Beibei Chen, Man He, Bin Hu
In this study, covalent triazine framework-1 (CTF-1) was adopted as solid phase extraction (SPE) sorbents, and a method of SPE inline coupled with high performance liquid chromatography-ultraviolet (HPLC-UV) detection was developed for trace analysis of three nitroimidazolaes (including metronidazole, ronidazole and dimetridazole) in porcine liver and environmental water samples. CTF-1 has rich π-electron and N containing triazine, thus can form π-π interaction and intermolecular hydrogen bond with three target polar nitroimidazoles, resulting in high extraction efficiency (87%-98%)...
February 3, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28007448/bioreductively-activatable-prodrug-conjugates-of-phenstatin-designed-to-target-tumor-hypoxia
#20
Blake A Winn, Zhe Shi, Graham J Carlson, Yifan Wang, Benson L Nguyen, Evan M Kelly, R David Ross, Ernest Hamel, David J Chaplin, Mary L Trawick, Kevin G Pinney
A variety of solid tumor cancers contain significant regions of hypoxia, which provide unique challenges for targeting by potent anticancer agents. Bioreductively activatable prodrug conjugates (BAPCs) represent a promising strategy for therapeutic intervention. BAPCs are designed to be biologically inert until they come into contact with low oxygen tension, at which point reductase enzyme mediated cleavage releases the parent anticancer agent in a tumor-specific manner. Phenstatin is a potent inhibitor of tubulin polymerization, mimicking the chemical structure and biological activity of the natural product combretastatin A-4...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
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