6 results about "Nitroimidazole derivatives" patented technology

The invention discloses application of a nitroimidazole derivative and a combined drug in preparation of a drug for resisting drug-sensitive tuberculosis, and belongs to the technical field of biological medicine. The invention provides application of a nitroimidazole derivative and a combined drug in preparation of a drug for resisting drug-sensitive tuberculosis in order to solve the clinical research blank of the nitroimidazole derivative in prevention and treatment of drug-sensitive tuberculosis. Animal experiments, I-stage clinic, II-stage clinic and medication dosage and mode optimization prove that the nitroimidazole derivative has no obvious drug accumulation, no obvious reproductive toxicity, no obvious cardiotoxicity and no QT interval extension, and compared with existing drugs such as deramanib, the nitroimidazole derivative is shorter in treatment time, more remarkable in curative effect, higher in safety and suitable for clinical application. Especially in lung iconography, voids of a patient are obviously reduced or focuses are obviously absorbed, so that the compound is expected to be used as a new medicine for preventing and treating drug-sensitive pulmonary tuberculosis.

The invention belongs to the field of medicinal chemistry, and particularly discloses a preparation method and application of a nitroimidazole derivative serving as an anti-tumor radiosensitizer. According to the invention, nitroimidazole is used as a lead compound, and a framework of nitroimidazole is modified through a series of reactions to obtain the novel nitroimidazole derivative. The compound can target a tumor hypoxia region, is reduced by a specific enzyme highly expressed in a hypoxia tumor tissue, and is combined with nucleophilic biological macromolecular free radicals generated by radiation to accelerate cancer cell death. As an anti-tumor radiosensitizer, the compound disclosed by the invention is expected to improve the tumor cell selectivity of the compound and reduce toxic and side effects, and is used for subsequent anti-tumor activity research.

The invention discloses a metal-based (copper or manganese) nitroimidazole derivative nano-enzyme as well as a preparation method and application thereof. After phenylboronic acid or dopamine is modified by a nitroimidazole skeleton, the nitroimidazole skeleton is complexed with metal ions to form nano-particles (NPs), so that the solubility of the nano-particles can be improved, various biological molecules and microorganisms can be combined in a targeted manner, the generation and evolution of drug-resistant strains can be weakened or inhibited, and the antibacterial activity can be enhanced. The preparation method is simple, the preparation conditions are mild, the operation is simple, the obtained copper-based nitroimidazole derivative nano-enzyme has excellent POD-like activity, the obtained manganese-based nitroimidazole derivative nano-enzyme has excellent CAT-like activity, and the two metal nano-enzymes both have good anti-staphylococcus aureus activity.

This invention discloses the use of a combination of nitroimidazole derivatives in the preparation of drugs for the prevention and treatment of drug-resistant tuberculosis, belonging to the field of biomedical technology. This invention fills the clinical research gap regarding the use of combination drugs of nitroimidazole derivatives in the prevention and treatment of drug-resistant tuberculosis, providing a method for its application in the preparation of drugs for this purpose. This invention demonstrates good therapeutic effects against drug-resistant tuberculosis by combining nitroimidazole derivatives with various other anti-tuberculosis drugs, and shows promise as a new drug for the prevention and treatment of drug-resistant tuberculosis.

The invention relates to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a D-proline modified 2-nitroimidazole derivative and application thereof. The radioactive preparation obtained by labeling the D-proline modified 2-nitroimidazole derivative with radionuclide is high in radiochemical purity and good in stability and has hypoxia selectivity. The compound has high uptake and good retention at tumor parts of tumor-bearing mice, the tumor / non-target ratio is high, the uptake of non-target organs such as liver and intestines is low, and the compound can be popularized and applied as a novel tumor hypoxia developer.

The present invention relates to the field of biopharmaceutical technology, and in particular, to use of a nitroimidazole derivative or a pharmaceutical combination in the preparation of a medicament against drug-sensitive tuberculosis. Animal studies, phase I and phase II clinical trials, and the optimization of dosage and route of administration have demonstrated that the nitroimidazole derivative has no significant drug accumulation, no significant reproductive toxicity, no significant cardiotoxicity, and no QT prolongation effects. Compared with existing drugs such as delamanid, the nitroimidazole derivative has shorter treatment time, more significant therapeutic effects, and higher safety. Especially in pulmonary images, the cavities in patients are significantly reduced, or the lesions are significantly absorbed, suggesting that the nitroimidazole derivative is promising as a novel drug for preventing and treating drug-sensitive tuberculosis.