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Nitroimidazoles

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https://www.readbyqxmd.com/read/29113731/oral-fexinidazole-for-late-stage-african-trypanosoma-brucei-gambiense-trypanosomiasis-a-pivotal-multicentre-randomised-non-inferiority-trial
#1
Victor Kande Betu Ku Mesu, Wilfried Mutombo Kalonji, Clélia Bardonneau, Olaf Valverde Mordt, Séverine Blesson, François Simon, Sophie Delhomme, Sonja Bernhard, Willy Kuziena, Jean-Pierre Fina Lubaki, Steven Lumeya Vuvu, Pathou Nganzobo Ngima, Hélène Mahenzi Mbembo, Médard Ilunga, Augustin Kasongo Bonama, Josué Amici Heradi, Jean Louis Lumaliza Solomo, Guylain Mandula, Lewis Kaninda Badibabi, Francis Regongbenga Dama, Papy Kavunga Lukula, Digas Ngolo Tete, Crispin Lumbala, Bruno Scherrer, Nathalie Strub-Wourgaft, Antoine Tarral
BACKGROUND: Few therapeutic options are available to treat late-stage human African trypanosomiasis, a neglected tropical disease caused by Trypanosoma brucei gambiense (g-HAT). The firstline treatment nifurtimox eflornithine combination therapy needs to be administered intravenously in a hospital setting by trained personnel, which is not optimal, given that patients often live in remote areas with few health resources. Therefore, we aimed to assess the safety and efficacy of an oral regimen of fexinidazole (a 2-substituted 5-nitroimidazole with proven trypanocidal activity) versus nifurtimox eflornithine combination therapy in patients with late-stage g-HAT...
November 3, 2017: Lancet
https://www.readbyqxmd.com/read/29100732/identification-of-nitroimidazole-oxime-derivatives-targeting-the-polo-box-domain-of-polo-like-kinase-1
#2
Juan Sun, Han-Yu Liu, Ruo-Fei Xu, Hai-Liang Zhu
Recent progress in the development of small molecular skeleton-derived polo-like kinase (PLK1) catalytic domain (KD) inhibitors has led to the synthesis of multiple ligands with high binding affinity. However, few systematic analyses have been conducted to identify key PLK1-PBD domain and characterize their interactions with potent PLK1 inhibitors. Therefore, we designed a series of PLK1-PBD inhibitors with an in silico scaffold modification strategy. A docking simulation combined with a primary screen in vitro were performed to filter for the lead compound, which was then substituted, synthesized and evaluated by a variety of bioassays...
October 28, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29096502/how-does-methylation-suppress-the-electron-induced-decomposition-of-1-methyl-nitroimidazoles
#3
F Kossoski, M T do N Varella
The efficient decomposition of nitroimidazoles (NIs) by low energy electrons is believed to underlie their radiosensitizing properties. Recent dissociative electron attachment (DEA) measurements showed that methylation at the N1 site unexpectedly suppresses the electron-induced reactions in 4(5)-NI. We report theoretical results that provide a clear interpretation of that astounding finding. Around 1.5 eV, DEA reactions into several fragments are initiated by a π(*) resonance, not considered in previous studies...
October 28, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/29089262/discovery-of-novel-nitroimidazole-enols-as-pseudomonas-aeruginosa-dna-cleavage-agents
#4
Zhen-Zhen Li, Lavanya Gopala, Vijai Kumar Reddy Tangadanchu, Wei-Wei Gao, Cheng-He Zhou
A series of nitroimidazole enols as new bacterial DNA-targeting agents were for the first time designed, synthesized and characterized by NMR, IR and HRMS spectra. The antimicrobial screening revealed that 2-methoxyphenyl nitroimidazole enol 3i possessed stronger anti-P. aeruginosa efficacy (MIC = 0.10 μmol/mL) than reference drugs Norfloxacin and Metronidazole. Time-kill kinetic assay manifested that the active molecule 3i could rapidly kill the tested strains. Molecular docking indicated that the interactions between compound 3i and topoisomerase II were driven by hydrogen bonds...
October 25, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29077920/metronidazole-an-update-on-metabolism-structure-cytotoxicity-and-resistance-mechanisms
#5
Simon A Dingsdag, Neil Hunter
Metronidazole, a nitroimidazole, remains a front-line choice for treatment of infections related to inflammatory disorders of the gastrointestinal tract including colitis linked to Clostridium difficile. Despite >60 years of research, the metabolism of metronidazole and associated cytotoxicity is not definitively characterized. Nitroimidazoles are prodrugs that are reductively activated (the nitro group is reduced) under low oxygen tension, leading to imidazole fragmentation and cytotoxicity. It remains unclear if nitroimidazole reduction (activation) contributes to the cytotoxicity profile, or whether subsequent fragmentation of the imidazole ring and formed metabolites alone mediate cytotoxicity...
October 25, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29059587/a-high-throughput-uhplc-method-for-the-analysis-of-5-nitroimidazole-residues-in-milk-based-on-salting-out-assisted-liquid-liquid-extraction
#6
Maykel Hernández-Mesa, Laura Carbonell-Rozas, Carmen Cruces-Blanco, Ana M García-Campaña
A novel salting-out assisted liquid-liquid extraction (SALLE) method has been developed for the extraction of eight 5-NDZ antibiotics from milk samples prior to their analysis by UHPLC. An exhaustive study of the parameters involved in the SALLE procedure has been carried out, optimizing the extraction solvent volume, the amount of the salt agent, and the centrifugation and vortex timing by an experimental design. After sample treatment, the obtained extract was reconstituted in the mobile phase (6:94 (v/v) acetonitrile/water containing 0...
October 13, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28993106/the-antitubercular-activity-of-various-nitro-triazole-imidazole-based-compounds
#7
Maria V Papadopoulou, William D Bloomer, Howard S Rosenzweig
Twenty three 3-nitrotriazole- and five nitroimidazole-based compounds, mostly amides, were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv (Mtb H37Rv) under aerobic or low oxygen conditions, intracellular activity in murine J774 macrophages or THP-1 cells, activity against resistant Mtb strains as well as cytotoxicity in normal cells. Compounds with a Minimum Inhibitory Concentration (MIC) less than 10μM and 10-50μM were characterized as active and moderately active, respectively, whereas compounds with a MIC >50μM were characterized inactive...
November 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28936509/x-ray-responsive-nanoparticles-with-triggered-release-of-nitrite-a-precursor-of-reactive-nitrogen-species-for-enhanced-cancer-radiosensitization
#8
Fang Liu, Junzhe Lou, Dimitre Hristov
Remotely and locally triggered release of therapeutic species by X-ray irradiation is highly desired to enhance the efficacy of radiotherapy. However, the development of such X-ray responsive nanosystems remains a challenge, especially in response to high energy clinically relevant X-ray radiation. Herein, we report novel nitroimidazole ligated gold nanoparticles (AuNPs) that synergistically function to release nitrite, an important precursor for nitric oxide and reactive nitrogen species that sensitize cancer cells, upon radiation with clinically used 6 MeV X-rays, while no release was detected without radiation...
October 5, 2017: Nanoscale
https://www.readbyqxmd.com/read/28919603/current-trends-of-using-antimicrobials-at-obstetrics-and-gynaecology-department-in-a-tertiary-care-hospital
#9
M M Islam, S K Saha, S Saha, U A Wahid, R R Gomes, K S Ahmed, A N Naushad, S E Suchi, C Saha, D Mondal
This cross-sectional descriptive study was done to analyse the current trends of using antimicrobials in various surgical procedures at Obstetrics and Gynaecology department in Mymensingh Medical College Hospital, Mymensingh from July 2014 to June 2015. Among 300 postoperative obstetrics and gynaecological surgery cases, samples were selected as non-random purposive selection method where pattern of using antimicrobials were analysed by SPSS method 20.1 versions. The incidence of antimicrobial resistance is on continued rise with a threat to return to the pre-antibiotic era...
July 2017: Mymensingh Medical Journal: MMJ
https://www.readbyqxmd.com/read/28919150/in-vitro-anti-tuberculosis-activity-of-azole-drugs-against-mycobacterium-tuberculosis-clinical-isolates
#10
Belén R Imperiale, Ángel A Cataldi, Nora S Morcillo
BACKGROUND: Latent tuberculosis has been associated with the persistence of dormant Mycobacterium tuberculosis in the organism of infected individuals, who are reservoirs of the bacilli and the source for spreading the disease in the community. New active anti-TB drugs exerting their metabolic action at different stages and on latent/dormant bacilli are urgently required to avoid endogenous reactivations and to be part of treatments of multi- and extensively-drug resistant tuberculosis (M/XDR-TB)...
September 14, 2017: Revista Argentina de Microbiología
https://www.readbyqxmd.com/read/28893784/dual-mechanism-of-action-of-5-nitro-1-10-phenanthroline-against-mycobacterium-tuberculosis
#11
Saqib Kidwai, Chan-Yong Park, Shradha Mawatwal, Prabhakar Tiwari, Myung Geun Jung, Tannu Priya Gosain, Pradeep Kumar, David Alland, Sandeep Kumar, Avinash Bajaj, Yun-Kyung Hwang, Chang Sik Song, Rohan Dhiman, Ill Young Lee, Ramandeep Singh
New chemotherapeutic agents with novel mechanisms of action are urgently required to combat the challenge imposed by the emergence of drug-resistant mycobacteria. In this study, a phenotypic whole-cell screen identified 5-nitro-1,10-phenanthroline (5NP) as a lead compound. 5NP-resistant isolates harbored mutations that were mapped to fbiB and were also resistant to the bicyclic nitroimidazole PA-824. Mechanistic studies confirmed that 5NP is activated in an F420-dependent manner, resulting in the formation of 1,10-phenanthroline and 1,10-phenanthrolin-5-amine as major metabolites in bacteria...
November 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28870526/drug-repurposing-strategy-against-trypanosoma-cruzi-infection-in-vitro-and-in-vivo-assessment-of-the-activity-of-metronidazole-in-mono-and-combined-therapy
#12
M R Simões-Silva, J S De Araújo, G M Oliveira, K C Demarque, R B Peres, I D'Almeida-Melo, D G J Batista, C F Da Silva, C Cardoso-Santos, P B Da Silva, M M Batista, M T Bahia, M N C Soeiro
Metronidazole (Mtz) is a commercial broad-spectrum nitroimidazolic derivative with relevant antimicrobial activity and relative safety profile. Therefore, it is fair to consider Mtz a candidate for drug repurposing for other neglected conditions such as Chagas disease (CD), a parasitic pathology caused by Trypanosoma cruzi. CD is treated only with benznidazole (Bz) and nifurtimox, both introduced in clinics decades ago despite important limitations, including low efficacy on the later disease stage (chronic form) and severe side effects...
September 7, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28867602/a-phase-3-double-blind-placebo-controlled-study-of-the-effectiveness-and-safety-of-single-oral-doses-of-secnidazole-2-g-for-the-treatment-of-women-with-bacterial-vaginosis
#13
Jane R Schwebke, Franklin G Morgan, William Koltun, Paul Nyirjesy
BACKGROUND: A novel single oral dose granule formulation of secnidazole 2 g, a 5-nitroimidazole with a longer half-life (∼17 hours) than metronidazole (∼8 hours), is being developed to treat bacterial vaginosis. OBJECTIVE: We sought to evaluate the effectiveness and safety of single-dose secnidazole 2 g compared to placebo for the treatment of women with bacterial vaginosis. STUDY DESIGN: In all, 189 women with bacterial vaginosis were randomized 2:1 to receive a single oral dose of secnidazole 2 g (N = 125) or matched placebo (N = 64) at 21 centers in the United States...
September 1, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28857685/enhanced-degradation-of-metronidazole-by-heterogeneous-sono-fenton-reaction-coupled-ultrasound-using-fe3o4-magnetic-nanoparticles
#14
Yang Hu, Guan Wang, Mingzhi Huang, Kairong Lin, Yuqiang Yi, Zhanqiang Fang, Pengjun Li, Kangming Wang
Metronidazole (MNZ), one of the most commonly used nitroimidazole antibiotics in the world, poses a serious threat to human life and health. In this study, an enhanced sono-Fenton process for the degradation of MNZ is presented. The catalytic capacity of nano-Fe3O4 in systems comprising ultrasound + Fe3O4 + H2O2, and the influential parameters such as H2O2, nano-Fe3O4 doses and pH for the Sono-Fenton process, was investigated. The results showed that the nano-Fe3O4 particles appeared to be roughly spherical in shape, with an average size of 10-20 nm...
August 31, 2017: Environmental Technology
https://www.readbyqxmd.com/read/28855472/analytical-method-for-nitroimidazoles-and-their-major-metabolites-in-livestock-and-fishery-products-using-lc-ms-ms
#15
Takatoshi Sakai, Satoru Nemoto, Reiko Teshima, Hiroshi Akiyama
A sensitive and reliable method for the simultaneous determination of four nitroimidazoles (ipronidazole (IPZ), dimetridazole (DMZ), metronidazole (MNZ) and ronidazole (RNZ)) and three metabolites (IPZ-OH, MNZ-OH and 2-hydroxymethyl-1-methyl-5-nitroimidazole (HMMNI)) in livestock and fishery products was developed. The analytes were extracted from samples with acetone containing acetic acid. The crude extracts were defatted by liquid-liquid partition using acetonitrile and n-hexane followed by solid-phase extraction using a cartridge column packed with divinylbenzene-N-vinylpyrolidone copolymer bearing sulfo groups...
2017: Shokuhin Eiseigaku Zasshi. Journal of the Food Hygienic Society of Japan
https://www.readbyqxmd.com/read/28822347/screening-and-confirmation-of-steroids-and-nitroimidazoles-in-urine-blood-and-food-matrices-sample-preparation-methods-and-liquid-chromatography-tandem-mass-spectrometric-separations
#16
Ádám Tölgyesi, Enikő Barta, Andrea Simon, Thomas J McDonald, Virender K Sharma
Veterinary drugs containing synthetic anabolic steroid and nitroimidazole active agents are not allowed for their applications in livestock of the European Union (EU). This paper presents analyses of twelve selected steroids and six nitroimidazole antibiotics at low levels (1.56μg/L-4.95μg/L and 0.17μg/kg-2.14μg/kg, respectively) in body fluids and egg incurred samples. Analyses involved clean-up procedures, high performance liquid chromatography (HPLC) separation, and tandem mass spectrometric screening and confirmatory methods...
October 25, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28805936/characterizing-hypoxia-in-human-glioma-a-simultaneous-multimodal-mri-and-pet-study
#17
Christine Preibisch, Kuangyu Shi, Anne Kluge, Mathias Lukas, Benedikt Wiestler, Jens Göttler, Jens Gempt, Florian Ringel, Mohamed Al Jaberi, Jürgen Schlegel, Bernhard Meyer, Claus Zimmer, Thomas Pyka, Stefan Förster
Hypoxia plays an important role for the prognosis and therapy response of cancer. Thus, hypoxia imaging would be a valuable tool for pre-therapeutic assessment of tumor malignancy. However, there is no standard validated technique for clinical application available yet. Therefore, we performed a study in 12 patients with high-grade glioma, where we directly compared the two currently most promising techniques, namely the MR-based relative oxygen extraction fraction (MR-rOEF) and the PET hypoxia marker H-1-(3-[(18) F]-fluoro-2-hydroxypropyl)-2-nitroimidazole ([(18) F]-FMISO)...
August 14, 2017: NMR in Biomedicine
https://www.readbyqxmd.com/read/28799237/anticancer-efficacy-of-the-hypoxia-activated-prodrug-evofosfamide-is-enhanced-in-combination-with-proapoptotic-receptor-agonists-against-osteosarcoma
#18
Vasilios Liapis, Aneta Zysk, Mark DeNichilo, Irene Zinonos, Shelley Hay, Vasilios Panagopoulos, Alexandra Shoubridge, Christopher Difelice, Vladimir Ponomarev, Wendy Ingman, Gerald J Atkins, David M Findlay, Andrew C W Zannettino, Andreas Evdokiou
Tumor hypoxia is a major cause of treatment failure for a variety of malignancies. However, hypoxia also leads to treatment opportunities as demonstrated by the development of compounds that target regions of hypoxia within tumors. Evofosfamide is a hypoxia-activated prodrug that is created by linking the hypoxia-seeking 2-nitroimidazole moiety to the cytotoxic bromo-isophosphoramide mustard (Br-IPM). When evofosfamide is delivered to hypoxic regions of tumors, the DNA cross-linking toxin, Br-IPM, is released leading to cell death...
September 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28793052/cordyceps-sinensis-promotes-immune-regulation-and-enhances-bacteriostatic-activity-of-pa-824-via-il-10-in-mycobacterium-tuberculosis-disease
#19
D G Li, Z X Ren
PA-824 is a novel bicyclic nitroimidazole anti-tuberculosis (TB) drug. Cordyceps sinensis (Berk.) Sacc. (CS) was proven to be a good immunomodulatory compound. This research aimed to investigate the effect of CS on PA-824 in Mycobacterium tuberculosis (M.tb) infected mice (female CBA/J mice, 6 to 8 weeks of age and 20±2 g of weight). Mice were randomly assigned to 4 groups: PA-824, CS, PA-824+CS, and control. To verify the effect of PA-824 and CS on M.tb, after drug administration, mice lungs were harvested and bacterial colony formations were measured...
August 7, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28771219/an-efficient-one-pot-catalyzed-synthesis-of-2-4-disubstituted-5-nitroimidazoles-displaying-antiparasitic-and-antibacterial-activities
#20
Fanny Mathias, Youssef Kabri, Liliane Okdah, Carole Di Giorgio, Jean-Marc Rolain, Cédric Spitz, Maxime D Crozet, Patrice Vanelle
A one-pot regioselective bis-Suzuki-Miyaura or Suzuki-Miyaura/Sonogashira reaction on 2,4-dibromo-1-methyl-5-nitro-1H-imidazole under microwave heating was developed. This method is applicable to a wide range of (hetero)arylboronic acids and terminal alkynes. Additionally, this approach provides a simple and efficient way to synthesize 2,4-disubstituted 5-nitroimidazole derivatives with antibacterial and antiparasitic properties.
August 3, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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