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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...
September 22, 2017: Nanoscale
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
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
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 chemotherapeutics agents with novel mechanism 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 mapped to fbiB and were also resistant to bicyclic nitroimidazole, PA-824. Mechanistic studies confirmed that 5NP is activated in F420 dependent manner resulting in formation of 1,10-phenanthroline and 1,10-phenanthrolin-5-amine as major metabolites in bacteria...
September 11, 2017: Antimicrobial Agents and Chemotherapy
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 1, 2017: Biochemical Pharmacology
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 (BV). OBJECTIVE: To evaluate the effectiveness and safety of single-dose secnidazole 2 g compared to placebo for the treatment of women with BV. STUDY DESIGN: 189 women with BV 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 US...
August 31, 2017: American Journal of Obstetrics and Gynecology
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
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
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
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
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
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
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
Maria V Papadopoulou, William D Bloomer, Howard S Rosenzweig, Marcel Kaiser
A limited number of novel 3-nitrotriazole- and 2-nitroimidazole-linked quinolines and quinazolines were synthesized and screened for in vitro antitrypanosomal and antitubercular activities as well as cytotoxicity in normal cells. All compounds were active against T. cruzi amastigotes, while all but one were active or moderately active against T. b. rhodesiense. However, only two chloroquinolines exhibited satisfactory selectivity indices (SI) against T. cruzi and only one of them demonstrated a satisfactory SI against T...
July 25, 2017: European Journal of Medicinal Chemistry
Eero Itälä, Katrin Tanzer, Sari Granroth, Kuno Kooser, Stephan Paul Denifl, Edwin Kukk
We present here the photofragmentation patterns of doubly ionized 4(5)-nitroimidazole and 1-methyl-5-nitroimidazole. The doubly ionized state was created by core ionizing the C 1s orbitals of the samples, rapidly followed by Auger decay. Due to the recent development of nitroimidazole-based radiosensitizing drugs, core ionization was selected as it represents the very same processes taking place under the irradiation with medical X-rays. In addition to the fragmentation patterns of the sample, we study the effects of methylation on the fragmentation patterns of nitroimidazoles...
August 1, 2017: Journal of Mass Spectrometry: JMS
Zohreh Fakhrieh Kashan, Mahdi Delavari, Mohsen Arbabi, Hossein Hooshyar
Trichomonas vaginalis is a flagellated parasite affecting about 276 million people annually worldwide. Tricomoniasis is associated with different complications in pregnant women and infants. 5'-nitroimidazole derivatives (metronidazole, ornidazole, and tinidazole) are FDA approved drugs recommended for trichomoniasis treatment. Treatment with metronidazole 5'-nitroimidazole derivatives is associated with many side effects, and drug resistance to metronidazole has been reported in some cases. Recently, many attempts have been made to evaluate the effects of plants on causative agents of vaginal infections...
September 2017: Iranian Biomedical Journal
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
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
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
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
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