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Qing Zhang, Qing Zhang, Yanxing Guan, Shaozheng Liu, Qingjie Chen, Xiangmin Li
BACKGROUND This study was specifically designed to develop a new 99mTc compound with 3-amino-4-[2-(2-methyl-5-nitro-1H-imidazol)-ethylamino]-4-oxo-butyrate (5-ntm-asp) and to verify whether this compound is feasible to be a radiopharmaceutical for hypoxic tumors. MATERIAL AND METHODS Metronidazole derivative 5-ntm-asp was synthesized and then radio-labeled by Na [99mTcO4], forming 99mTc-5-ntm-asp. Another two complexes of 99mTc-2- and 99mTc-5-nitroimidazole-iminodiacetic acid (99mTc-2-ntm-IDA and 99mTc-5-ntm-IDA) were also synthesized based on previous studies...
October 18, 2016: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Nan Lu, Ting Wang, Pan Zhao, Lianjun Zhang, Xiaowen Lun, Xueli Zhang, Xiaohong Hou
In the presented work, metal-organic framework (MOF) material MIL-101(Cr) (MIL, Matérial Institute Lavoisier) was used as a sorbent for vortex assisted dispersive micro-solid-phase extraction (VA-D-μ-SPE) of trace amount of metronidazole (MNZ), ronidazole (RNZ), secnidazole (SNZ), dimetridazole (DMZ), tinidazole (TNZ), and ornidazole (ONZ) in different environmental water samples. Ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) was used to quantify the target analytes...
October 8, 2016: Analytical and Bioanalytical Chemistry
Nitya Sarjapuram, Niharika Mekala, Meetali Singh, Utpal Tatu
Travellers' diarrhoea caused by enteric protozoa like Entamoeba histolytica is among the most common protozoan diseases in developing countries. In developing countries, amoebiasis is the second most prevalent protozoan disease. This protozoan parasite is often known to coexist as a part of the normal gut microbiota. It is estimated that around 50-60 % of population in developing countries might be harbouring Entamoeba in an asymptomatic manner. Due to physiological perturbation or upon immuno-compromise, it can become virulent and then cause diarrhoea, bloody stools and may invade other organs if left untreated...
October 5, 2016: Probiotics and Antimicrobial Proteins
Claudia Karnthaler-Benbakka, Diana Groza, Bettina Koblmüller, Alessio Terenzi, Katharina Holste, Melanie Haider, Dina Baier, Walter Berger, Petra Heffeter, Christian R Kowol, Bernhard K Keppler
Tyrosine kinase inhibitors (TKIs), which have revolutionized cancer therapy over the past 15 years, are limited in their clinical application due to serious side effects. Therefore, we converted two approved TKIs (sunitinib and erlotinib) into 2-nitroimidazole-based hypoxia-activatable prodrugs. Kinetics studies showed very different stabilities over 24 h; however, fast reductive activation via E. coli nitroreductase could be confirmed for both panels. The anticancer activity and signaling inhibition of the compounds against various human cancer cell lines were evaluated in cell culture...
October 5, 2016: ChemMedChem
Wen-Juan Huang, Wei-Wei Chen, Xia Zhang
Central nervous system-based cancers have a much higher mortality rate with the 2016 estimates at 6.4 for incidence and 4.3 for deaths per 100,000 individuals. Grade IV astrocytomas, known as glioblastomas are highly aggressive and show a high proliferation index, diffused infiltration, angiogenesis, microvascular proliferation and pleomorphic vessels, resistance to apoptosis, and pseudopalisading necrosis. Extensive hypoxic regions in glioblastomas contribute to the highly malignant phenotype of these tumors...
October 2016: Oncology Letters
Chinnasamy Kalaiarasi, Mysore S Pavan, Poomani Kumaradhas
An experimental charge density distribution of 2-nitroimidazole was determined from high-resolution X-ray diffraction and the Hansen-Coppens multipole model. The 2-nitroimidazole compound was crystallized and a high-angle X-ray diffraction intensity data set has been collected at low temperature (110 K). The structure was solved and further, an aspherical multipole model refinement was performed up to octapole level; the results were used to determine the structure, bond topological and electrostatic properties of the molecule...
October 1, 2016: Acta Crystallographica Section B, Structural Science, Crystal Engineering and Materials
Patrícia de Brum Vieira, Tiana Tasca, W Evan Secor
Trichomoniasis is a sexually transmitted disease (STD) caused by infection with the protozoan parasite Trichomonas vaginalis. It is considered the most prevalent non-viral sexually transmitted disease worldwide. Recently, the infection has been associated with adverse outcomes of pregnancy and increased risks of HIV acquisition and transmission, besides the association with cervical and prostate cancers. The consequences of trichomoniasis are likely much greater than previously recognized, both at the individual and the community level...
September 30, 2016: Current Topics in Medicinal Chemistry
Anna Schweifer, Florian Maier, Walter Ehrlichmann, Denis Lamparter, Manfred Kneilling, Bernd J Pichler, Friedrich Hammerschmidt, Gerald Reischl
INTRODUCTION: Radiolabeled 2-nitroimidazoles (azomycins) are a prominent class of biomarkers for PET imaging of hypoxia. [(18)F]Fluoro-azomycin-α-arabinoside ([(18)F]FAZA) - already in clinical use - may be seen as α-configuration nucleoside, but enters cells only via diffusion and is not transported by cellular nucleoside transporters. To enhance image contrast in comparison to [(18)F]FAZA our objective was to (18)F-radiolabel an azomycin-2´-deoxyriboside with β-configuration ([(18)F]FAZDR, [(18)F]-β-8) to mimic nucleosides more closely and comparatively evaluate it versus [(18)F]FAZA...
August 9, 2016: Nuclear Medicine and Biology
Asitha Abeywardane, Gary Caviness, Younggi Choi, Derek Cogan, Amy Gao, Daniel Goldberg, Alexander Heim-Riether, Debra Jeanfavre, Elliott Klein, Jennifer A Kowalski, Wang Mao, Craig Miller, Neil Moss, Philip Ramsden, Ernest Raymond, Donna Skow, Lana Smith-Keenan, Roger J Snow, Frank Wu, Jiang-Ping Wu, Yang Yu
Compound 1 ((4-amino-3,5-dichlorophenyl)-1-(4-methylpiperidin-1-yl)-4-(2-nitroimidazol-1-yl)-1-oxobutane-2-sulfonamido) was discovered to be a 690nM antagonist of human CCR10 Ca(2+) flux. Optimization delivered (2R)-4-(2-cyanopyrrol-1-yl)-S-(1H-indol-4-yl)-1-(4-methylpiperidin-1-yl)-1-oxobutane-2-sulfonamido (eut-22) that is 300 fold more potent a CCR10 antagonist than 1 and eliminates potential toxicity, mutagenicity, and drug-drug-interaction liabilities often associated with nitroaryls and anilines. eut-22 is highly selective over other GPCR's, including a number of other chemokine receptors...
September 21, 2016: Bioorganic & Medicinal Chemistry Letters
Zhiwen Zhang, Yuping Wu, Xiaowei Li, Yingyu Wang, Hui Li, Qin Fu, Yawen Shan, Tianhe Liu, Xi Xia
This study describes the development of a multiresidue method for the efficient identification and quantification of nitroimidazoles, nitrofurans, and chloramphenicol in chicken and egg. After derivatization of nitrofuran metabolites, dispersive-solid phase extraction was used for the extraction of target analytes. An optimization strategy involved the selection of sorbents and extraction solutions for dispersive-solid phase extraction in order to achieve acceptably high recoveries and reduce co-extractives in the final extracts...
February 15, 2017: Food Chemistry
Yehouda Marcus, Noam Tal, Mordechai Ronen, Raanan Carmieli, Michael Gurevitz
Ornidazole of the 5-nitroimidazole drug family is used to treat protozoan and anaerobic bacterial infections via a mechanism that involves pre-activation by reduction of the nitro group, and production of toxic derivatives and radicals. Metronidazole, another drug family member, has been suggested to affect photosynthesis by draining electrons from the electron carrier, ferredoxin, thus inhibiting NADP(+) reduction and stimulating radical and peroxide production. Here we show, however, that ornidazole inhibits photosynthesis via a different mechanism...
September 19, 2016: Biochemical Journal
Ryohsuke Kurihara, Yuta Ikemura, Kazuhito Tanabe
Hypoxia is a characteristic feature of solid tumors. Herein, we have developed novel hypoxia-sensitive probes (IM-ACs) for Raman spectroscopic analysis, consisting of nitroimidazole as a hypoxia-targeting unit and acetylene group as the signal-emitting unit. Among IM-ACs synthesized in this study, IM-AC possessing a diacetylene group (IM-AC 3), showed suitable properties as a hypoxia indicator. When administered to A549 cells, we observed a strong signal of IM-AC 3 around 2200cm(-1) in the Raman spectra from hypoxic cells...
October 15, 2016: Bioorganic & Medicinal Chemistry Letters
Dhanaraju Mandalapu, Bhavana Kushwaha, Sonal Gupta, Nidhi Singh, Mahendra Shukla, Jitendra Kumar, Dilip K Tanpula, Satya N Sankhwar, Jagdamba P Maikhuri, Mohammad I Siddiqi, Jawahar Lal, Gopal Gupta, Vishnu L Sharma
Trichomoniasis is the most prevalent, non-viral sexually transmitted diseases (STD) caused by amitochondriate protozoan Trichomonas vaginalis. Increased resistance of T. vaginalis to the marketed drug Metronidazole necessitates the development of newer chemical entities. A library of sixty 2-methyl-4/5-nitroimidazole derivatives was synthesized via nucleophilic ring opening reaction of epoxide and the efficacies against drug-susceptible and -resistant Trichomonas vaginalis were evaluated. All the molecules except two were found to be active against both susceptible and resistant strains with MICs ranging 8...
September 4, 2016: European Journal of Medicinal Chemistry
Thomas Wanek, Katharina Kreis, Petra Križková, Anna Schweifer, Christoph Denk, Johann Stanek, Severin Mairinger, Thomas Filip, Michael Sauberer, Patricia Edelhofer, Alexander Traxl, Viktoria E Muchitsch, Kurt Mereiter, Friedrich Hammerschmidt, Carol E Cass, Vijaya L Damaraju, Oliver Langer, Claudia Kuntner
Positron emission tomography (PET) using fluorine-18 ((18)F)-labeled 2-nitroimidazole radiotracers has proven useful for assessment of tumor oxygenation. However, the passive diffusion-driven cellular uptake of currently available radiotracers results in slow kinetics and low tumor-to-background ratios. With the aim to develop a compound that is actively transported into cells, 1-(6'-deoxy-6'-[(18)F]fluoro-β-d-allofuranosyl)-2-nitroimidazole (β-[(18)F]1), a putative nucleoside transporter substrate, was synthetized by nucleophilic [(18)F]fluoride substitution of an acetyl protected labeling precursor with a tosylate leaving group (β-6) in a final radiochemical yield of 12±8% (n=10, based on [(18)F]fluoride starting activity) in a total synthesis time of 60min with a specific activity at end of synthesis of 218±58GBq/μmol (n=10)...
November 1, 2016: Bioorganic & Medicinal Chemistry
Aziz Filali-Ansary, Cécile Augé, Audrey Abgrall, Marie Souchaud, Franck Pellissier, Olaf Valverde Mordt, Séverine Blesson, Ger-Jan Sanderink
AIM: Fexinidazole (FEX) is a nitroimidazole being developed as a new trypanocide treatment for human African trypanosomiasis/sleeping sickness. Its main metabolites, fexinidazole sulfoxide (M1) and fexinidazole sulfone (M2), show the same in vitro pharmacological activity as FEX. METHODS & RESULTS: An LC-MS/MS assay was developed for quantitation of FEX in DBS, collected via finger-prick from healthy subjects. The DBS assay was specific, accurate and reproducible for FEX, M1 and M2 when validated against the current plasma assay...
October 2016: Bioanalysis
Yukiko Masaki, Yoichi Shimizu, Takeshi Yoshioka, Fei Feng, Songji Zhao, Kenichi Higashino, Yoshito Numata, Yuji Kuge
Hypoxia, or low oxygen concentration, is a key factor promoting tumor progression and angiogenesis and resistance of cancer to radiotherapy and chemotherapy. 2-Nitroimidazole-based agents have been widely used in pathological and nuclear medicine examinations to detect hypoxic regions in tumors; in particular, pimonidazole is used for histochemical staining of hypoxic regions. It is considered to accumulate in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group...
2016: PloS One
Lin Kang, Bo Fan, Ping Sun, Wei Huang, Mingji Jin, Qiming Wang, Zhonggao Gao
UNLABELLED: Hypoxia is a feature of most solid tumors, targeting hypoxia is considered as the best validated yet not extensively exploited strategy in cancer therapy. Here, we reported a novel tumor-targeting strategy using a hypoxia-sensitive siRNA delivery system. In the study, 2-nitroimidazole (NI), a hydrophobic component that can be converted to hydrophilic 2-aminoimidazole (AI) through bioreduction under hypoxic conditions, was conjugated to the alkylated polyethyleneimine (bPEI1...
October 15, 2016: Acta Biomaterialia
Eva Ramos, Joseba Santamaría, Gorka Santamaría, Luis Barbier, Icíar Arteagoitia
OBJECTIVES: The use of antibiotics to prevent dry socket and infection is a controversial but widespread practice. The aim of the study is to assess the efficacy of systemic antibiotics in reducing the frequencies of these complications after extraction. STUDY DESIGN: A systematic review and meta-analysis, according to the PRISMA statement, based on randomized double-blind placebo-controlled trials evaluating systemic antibiotics to prevent dry socket and infection after third molar surgery...
October 2016: Oral Surgery, Oral Medicine, Oral Pathology and Oral Radiology
Gurleen Kour, Anil Kumar, Parvinder Pal Singh, Sumit Sharma, Asha Bhagat, Ram A Vishwakarma, Zabeer Ahmed
New compounds against tuberculosis are urgently needed to combat the crisis of drug resistance in tuberculosis (TB). We have identified a nitrodihydroimidazooxazole analog, IIIM-019 as a new anti-tubercular agent with a MIC of 0.23 μM against H37Rv. Physicochemical properties, in-vitro pharmacokinetics and in-vivo multiple-doses pharmacokinetics were studied for the compound. In silico physicochemical parameters and Lipinski's violations were determined for drug like properties. Lipophilicity was determined experimentally as Octanol-PBS partition coefficient (log P)...
October 2016: Pulmonary Pharmacology & Therapeutics
Diego Airado-Rodríguez, Maykel Hernández-Mesa, Ana M García-Campaña, Carmen Cruces-Blanco
A methodology is presented for the sensitive determination of nitromidazole residues in egg by means of micellar electrokinetic capillary chromatography in combination with cation selective exhaustive injection and ultraviolet detection. Six compounds have been considered and the separation has been achieved in less than 12min in a 61.5-cm effective length capillary with 50-μm internal diameter. Phosphate buffer 44mM pH 2.5, containing 8% tetrahydrofurane and 123mM sodium dodecyl sulfate was employed as running buffer...
December 15, 2016: Food Chemistry
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