The depletion of three banned nitroimidazole drugs - dimetridazole (DMZ), metronidazole (MNZ) and ronidazole (RNZ) - was investigated in black tiger shrimp (Penaeus monodon) following in-water medication. The highest concentrations of residues were measured immediately after the 24-h immersion (d0). At this time, MNZ and MNZ-OH residues were measured in shrimp tissue samples at concentrations r...

Since observations from the beginning of the last century, it has become well established that solid tumors may contain oxygen-deficient hypoxic areas and that cells in such areas may cause tumors to become radioresistant. Identifying hypoxic cells in human tumors has improved by the help of new imaging and physiologic techniques, and a substantial amount of data indicates the presence of hypox...

The antibacterial activities of different nitroheterocyclic compounds were assessed by an agar dilution method against aerobic, microaerophilic, and anaerobic bacteria. Nitronaphthofurans inhibited the multiplication of aerobic bacteria at low concentrations (MIC for 50% of strains tested [MIC50], 1 mg/liter). Under anaerobic growth conditions the MICs were found to be even lower. The rough, DN...

The radiosensitizing effects of PR-350, a nitroimidazole derivative, were examined concerning the cell killing of human pancreatic cancer cell lines exposed to high doses of gamma-ray irradiation in vitro. The percentages of dead cells were analyzed with a multiwell plate reader to measure the fluorescence intensity of propidium iodide before and after a digitonin treatment. The sensitizing eff...

Inhibitory activities of monocyclic nitroimidazoles against Mycobacterium tuberculosis (Mtb) deazaflavin-dependent nitroreductase (DDN) were modeled by using docking, pharmacophore alignment and comparative molecular similarity indices analysis (CoMSIA) methods. A statistically significant model obtained from CoMSIA was established based on a training set using pharmacophore-based molecular ali...

This paper provides quantitative structure activity relationship (QSAR) models for predicting the radiosensitization effectiveness of nitroimidazole compounds. A new method, combining a heuristic method and projection pursuit regression, was used to build an advanced QSAR model. Compared to the conventional multi-linear regression model, this model showed better predictive ability and reliabili...

Nitroimidazoles have been shown to be the drugs of choice to treat women with bacterial vaginosis, but the recurrence rate is high. Some workers have suggested that the recurrence of symptoms may in fact be reinfection by male consorts, but no controlled studies have been undertaken to confirm this. In an international, multicentre, randomised, double blind trial, the recurrence rate was studie...

OBJECTIVE Multiple-dose metronidazole oral therapy is currently the reference treatment for bacterial vaginosis (BV). This double-blind, double-dummy, noninferiority study compared the efficacy of secnidazole, another nitroimidazole with pharmacokinetics allowing a single dose regimen, to this standard treatment. METHODS A total of 577 patients were randomized to receive metronidazole (500 mg...

New imidazole-based energetic molecules (1,4-dinitroimidazole, 2,4-dinitroimidazole, 1-methyl-2,4-dinitroimidazole, and 1-methyl-2,4,5-trinitroimidazole) are studied both experimentally and theoretically. The NO molecule is observed as a main decomposition product from the above nitroimidazole energetic molecules excited at three UV wavelengths (226, 236, and 248 nm). Resolved rotational spectr...