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Javier Giglio et al.
Nuclear medicine and biology, 39(5), 679-686 (2012-04-27)
The evaluation of oxygenation status of solid tumors is an important field of radiopharmaceutical research. With the aim to develop new potential 99mTc-radiopharmaceuticals for imaging hypoxia, we have synthesized two novel isocyanide derivatives of metronidazole, which has demonstrated high affinity
Pandurang M Jadhav et al.
Journal of molecular modeling, 19(8), 3027-3033 (2013-04-12)
1-Methyl-2,4,5-trinitro imidazole (MTNI) is a well-known melt cast explosive possessing good thermal stability and impact insensitivity. MTNI has been synthesized from multi-step nitration followed by methylation of imidazole exhibiting low yield. It is desirable to screen the process thermodynamically for
E Cambau et al.
Revue scientifique et technique (International Office of Epizootics), 31(1), 77-87 (2012-08-02)
Several antimicrobials act by inhibiting the synthesis of nucleic acids (rifamycins, sulfamides, diaminopyridines), modifying their conformation (quinolones, coumarins) or causing irreversible lesions (nitroimidazoles, nitrofurans). The resistance mechanisms are: a reduction in intracytoplasmic accumulation, modification of the target or the production
Meral Uyar et al.
Respirology (Carlton, Vic.), 14(4), 612-613 (2009-08-04)
Diffuse alveolar haemorrhage (DAH) is indicated by the presence of red blood cells, fibrin and haemosiderin deposits in the lung parenchyma. We present a case of DAH in a 25-year-old male following 5-nitroimidazole treatment. The first episode of haemoptysis occurred
Anil Bidwai et al.
Biochimica et biophysica acta, 1854(8), 919-929 (2015-04-23)
Imidazole binding to three apolar distal heme pocket mutants of yeast cytochrome c peroxidase (CcP) has been investigated between pH4 and 8. The three CcP variants have Arg-48, Trp-51, and His-52 mutated to either all alanine, CcP(triAla), all valine, CcP(triVal)
Javier Giglio et al.
Bioorganic & medicinal chemistry letters, 21(1), 394-397 (2010-11-23)
With the aim to develop new potential (99m)Tc-radiopharmaceuticals for imaging hypoxia based on the formation of Tc-nitrido complexes, two novel dithiocarbamate containing metronidazole derivatives (L1 and L2) have been prepared and characterised. The synthesis of L1 and L2 was achieved
Taosheng Chen et al.
Assay and drug development technologies, 4(4), 387-396 (2006-09-02)
Receptor activator of nuclear factor-kappaB (NF-kappaB) (RANK) plays a key role in the differentiation, activation, and survival of osteoclasts. Upon activation of RANK with RANK ligand (RANKL), osteoclast precursor cells differentiate into tartrate-resistant acid phosphatase (TRAP)-positive, multinucleated osteoclasts. To identify
Maciej Kubicki et al.
Acta crystallographica. Section C, Crystal structure communications, 63(Pt 8), o454-o457 (2007-08-07)
In the crystal structures of the two imidazole derivatives 5-chloro-1,2-dimethyl-4-nitro-1H-imidazole, C(5)H(6)ClN(3)O(2), (I), and 2-chloro-1-methyl-4-nitro-1H-imidazole, C(4)H(4)ClN(3)O(2), (II), C-Cl...O halogen bonds are the principal specific interactions responsible for the crystal packing. Two different halogen-bond modes are observed: in (I), there is one
Soledad Fernández et al.
Bioorganic & medicinal chemistry, 20(13), 4040-4048 (2012-06-05)
An important issue in the development of metal-based radiopharmaceuticals is the selection of the labelling strategy in order to couple the metal to the pharmacophore without losing the biological activity. With the aim to evaluate the correlation between ligand denticity
Thierry Juspin et al.
Molecules (Basel, Switzerland), 16(8), 6883-6993 (2011-08-16)
We report herein the synthesis of substituted 2-[4-(1,2-dimethyl-5-nitro-1H-imidazol-4-yl)phenyl]-1-arylethanols, ethyl 3-[4-(1,2-dimethyl-5-nitro-1H-imidazol-4-yl)-phenyl]-2-hydroxypropanoate and 2-[4-(1,2-dimethyl-5-nitro-1H-imidazol-4-yl)benzyl]-2-hydroxy-acenaphthylen-1(2H)-one from the reactions of 4-[4-(chloromethyl)phenyl]-1,2-dimethyl-5-nitro-1H-imidazole with various aromatic carbonyl and a-carbonyl ester derivatives using tetrakis(dimethylamino)ethylene (TDAE) methodology.
David Leitsch et al.
The Journal of antimicrobial chemotherapy, 66(8), 1756-1765 (2011-05-24)
The mechanism of action of, and resistance to, metronidazole in the anaerobic (or micro-aerotolerant) protozoan parasite Giardia lamblia has long been associated with the reduction of ferredoxin (Fd) by the enzyme pyruvate:ferredoxin oxidoreductase (PFOR) and the subsequent activation of metronidazole
Raúl Argüello-García et al.
Infection, genetics and evolution : journal of molecular epidemiology and evolutionary genetics in infectious diseases, 9(6), 1057-1064 (2009-06-02)
The susceptibility of Giardia duodenalis trophozoites exposed in vitro to sublethal concentrations of metronidazole (MTZ) and albendazole (ABZ) may exhibit inter-culture (variability) and intra-culture (variation) differences in drug susceptibility. It was previously reported that MTZ-resistant trophozoites may display changes in
Heterocyclic compounds as catalysts in the peroxyoxalate chemiluminescence reaction of bis (2, 4, 6-trichlorophenyl) oxalate.
Jonsson T and Irgum K.
Analytica Chimica Acta, 361(3), 205-215 (1998)
Pascal Mottier et al.
Journal of agricultural and food chemistry, 54(6), 2018-2026 (2006-03-16)
An isotope dilution liquid chromatography-electrospray ionization-tandem mass spectrometry method is presented for the simultaneous analysis of several 5-nitroimidazole-based veterinary drugs, which are dimetridazole (DMZ), ronidazole (RNZ), metronidazole (MNZ), ipronidazole (IPZ), and their hydroxylated metabolites (DMZOH, MNZOH, and IPZOH), in egg
Yukiko Miyamoto et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(43), 17564-17569 (2013-10-09)
Metronidazole and other 5-nitroimidazoles (5-NI) are among the most effective antimicrobials available against many important anaerobic pathogens, but evolving resistance is threatening their long-term clinical utility. The common 5-NIs were developed decades ago, yet little 5-NI drug development has since
Haythem A Saadeh et al.
Molecules (Basel, Switzerland), 14(8), 2758-2767 (2009-08-25)
A number of 5-aryl-1-methyl-4-nitroimidazoles 5a-f have been synthesized in good yields by the Suzuki coupling reaction between 5-chloro-1-methyl-4-nitroimidazole (3) and arylboronic acids 4a-f, aided by dichlorobis-(triphenylphosphine)palladium(II), K(2)CO(3, )and tetrabutylammonium bromide in water at 70-80 degrees C. Compounds 5a-f were characterized
N S Makhlaĭ et al.
Zhurnal mikrobiologii, epidemiologii, i immunobiologii, (3)(3), 71-75 (2011-08-04)
Development of test system for the evaluation of sensitivity of Trichomonas vaginalis to preparations of the 5-nitroimidazole and 5-nitrofuran groups. Determination of minimal cidic concentration (MCC) of antiprotozoal preparations was carried out by cultivating laboratory T. vaginalis strains in wells
Carlos A Valdez et al.
Journal of medicinal chemistry, 52(13), 4038-4053 (2009-06-02)
Infections with the diarrheagenic pathogen, Giardia lamblia, are commonly treated with the 5-nitroimidazole (5-NI) metronidazole (Mz), and yet treatment failures and Mz resistance occur. Using a panel of new 2-ethenyl and 2-ethanyl 5-NI derivatives, we found that compounds with a
Soledad Fernández et al.
Nuclear medicine and biology, 40(2), 273-279 (2012-12-12)
Hypoxia imaging is an important field in radiopharmaceutical research since hypoxic cells are very resistant to radiation treatment and diffusional limitations restrict the efficacy of chemotherapy. Gallium-68 is a widely used radionuclide for positron emission tomography (PET) due to the
Rayane Mohamed et al.
Journal of agricultural and food chemistry, 56(10), 3500-3508 (2008-05-07)
A nitroimidazole, molecularly imprinted polymer (MIP) was tested to extract four 5-nitroimidazoles (i.e., dimetridazole (DMZ), ipronidazole (IPZ), metronidazole (MNZ), and ronidazole (RNZ)) and three of their metabolites (i.e., DMZOH, IPZOH, and MNZOH) from egg powder samples. Various MIP templates were
J Chacko et al.
Neurology India, 59(5), 743-747 (2011-10-25)
We report two patients manifesting with involvement of central and peripheral nervous system with brain magnetic resonance imaging (MRI) changes and pathological features of neuropathy possibly due to harmful and chronic use of various nitroimidazole group of medications for recurrent
Mohammad Hassan Moshafi et al.
Archiv der Pharmazie, 344(3), 178-183 (2011-03-09)
A series of 5-nitroimidazole-based 1,3,4-thiadiazoles were prepared and tested for antibacterial activity against Helicobacter pylori. The anti-H. pylori activity of target compounds along with the commercially available antimicrobial metronidazole was evaluated by comparing the inhibition-zone diameters determined by the paper
Maxime D Crozet et al.
European journal of medicinal chemistry, 44(2), 653-659 (2008-07-02)
To improve the antiparasitic pharmacophore, 20 5-nitroimidazoles bearing an arylsulfonylmethyl group were prepared from commercial imidazoles. The antiparasitic activity of these molecules was assessed against Trichomonas vaginalis, the in vitro cytotoxicity was evaluated on human monocytes and the mutagenicity was
Sequential regimens for Helicobacter pylori eradication.
Paul Moayyedi
Lancet (London, England), 370(9592), 1010-1012 (2007-09-25)
James E Erman et al.
Biochimica et biophysica acta, 1854(8), 869-881 (2015-04-25)
Imidazole, 1-methylimidazole and 4-nitroimidazole bind to yeast cytochrome c peroxidase (yCcP) with apparent equilibrium dissociation constants (KD(app)) of 3.3±0.4, 0.85±0.11, and ~0.2M, respectively, at pH7. This is the weakest imidazole binding to a heme protein reported to date and it
Linda A Dunn et al.
International journal of antimicrobial agents, 36(1), 37-42 (2010-05-12)
The 5-nitroimidazole (NI) compound C17, with a side chain carrying a remote phenyl group in the 2-position of the imidazole ring, is at least 14-fold more active against the gut protozoan parasite Giardialamblia than the 5-NI drug metronidazole (MTR), with
Hanna-Kirsti S Leiros et al.
The Journal of biological chemistry, 279(53), 55840-55849 (2004-10-20)
5-Nitroimidazole-based antibiotics are compounds extensively used for treating infections in humans and animals caused by several important pathogens. They are administered as prodrugs, and their activation depends upon an anaerobic 1-electron reduction of the nitro group by a reduction pathway
S Kovachev et al.
Akusherstvo i ginekologiia, 50(3), 30-36 (2011-09-16)
The aim of this study is to investigate the effectiveness of short-term, combined 5-nitroimidazole treatment in vaginal dysbacteriosis with dominant anaerobic species. The presence of infection was proven by microscopic examination of vaginal fluid (Nugent, modified by Ison-Hay-Keane scale), microbiological
Claire Ceballos et al.
Bioconjugate chemistry, 21(6), 1062-1069 (2010-05-21)
Cationic nucleoside lipids (CNLs) derived from 5-nitroindole and 4-nitroimidazole bases were prepared from d-ribose by using a straightforward chemical synthesis. TEM experiments indicate that these amphiphilic molecules self-assemble to form supramolecular organizations in aqueous solutions. Electrophoresis and standard ethidium bromide
Dorota Olender et al.
European journal of medicinal chemistry, 44(2), 645-652 (2008-07-02)
Some new nitroimidazole derivatives have been synthesized by treating 4,5-dinitro- and 2-methyl-4,5-dinitroimidazoles with epoxypropane, epichlorohydrin or phenacyl bromide in alkylation reactions. The nitro group in N-substituted 4,5-dinitro- and 2-methyl-4,5-dinitroimidazoles has been replaced with primary and secondary amines to afford 4-amino-5-nitroimidazole
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