Abstract
Many interesting applications have been found for nitroimidazoles as therapeutic agents. Among others, some of these compounds can radiosensitize hypoxic tumor cells. The introduction of a second nitroimidazole ring to the molecule can improve the level of its pharmacological effect. The aim of this article is to overview the literature concerning active compounds that contain two nitroimidazole moieties in their structures.
Highlights
The antibiotic azomycin was the first active nitroimidazole to be discovered [1]
This research led to the acquisition of the 5-nitroimidazole derivative—metronidazole, which is most widely used in the treatment of anaerobic protozoan parasitic infections caused by Trichomonas vaginalis, Giardia duodenalis, and Entamoeba histolytica [2,3]
Misonidazole, metronidazole, and etanidazole were placed in the group of the first nitroimidazole derivatives tested in clinical trials
Summary
The antibiotic azomycin was the first active nitroimidazole to be discovered [1]. Its discovery provided the major impulse for the systematic search for medicines showing activity against anaerobic protozoa. In the absence of an adequate supply of O2 , in hypoxic tissue, they undergo further reduction to more reactive products that bind to cell components because the decreased oxygen concentration is not able to effectively compete to reoxidize the molecule. Reduction takes place in all tissues with viable enzymatic processes, but retention only exists in those tissues with reduced oxygen levels In addition to their radiosensitizing activity, nitroimidazole derivatives are selectively toxic to hypoxic cells because of their reductive activation via oxygen-inhibitable metabolic pathways [9]. One of the most investigated types of compounds are 2-nitroimidazole derivatives They undergo enzymic, oxygen-inhibitable reduction of NO2 group, resulting in preferential metabolism in hypoxic cells to reactive metabolites [10]. SPECT/CT imaging confirmed that the tumors could be visualized clearly with comp. 18 at 2 h (conc. 22% ID/g)
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