Disease relevance of NSC50359

• Structural basis of 5-nitroimidazole antibiotic resistance: the crystal structure of NimA from Deinococcus radiodurans [1].
• Either gene may confer 5-nitroimidazole resistance to susceptible strains of Bacteroides [2].
• Satranidazole, a 5-nitroimidazole derivative, was tested for its activity against reference strains and clinical isolates of anaerobic bacteria in vitro and in two murine models of anaerobic infection in comparison with metronidazole, tinidazole, ornidazole and clindamycin [3].
• Reduction of 2-, 4- and 5-nitroimidazole drugs by hydrogenase 1 in Clostridium pasteurianum [4].
• Response of the solid Guerin epitheliomas of rats to fractionated irradiation and a new 4-nitroimidazole [5].

High impact information on NSC50359

• By contrast, a curative regimen of melaminylthioarsenite and 5-nitroimidazole, which cleared parasites from the central nervous system, did not cause any pathological reaction in the mice [6].
• Metronidazole (Mz)-resistant Giardia and Trichomonas were inhibited by 1 of 30 new 5-nitroimidazole drugs [7].
• These results agree with those found for the QSAR of 5-nitroimidazole analogues [8].
• Unlabeled misonidazole, a 2-nitroimidazole, inhibited accumulation of radioactivity, whereas tinidazole, a 5-nitroimidazole, enhanced accumulation; similar effects had been reported with BMS181321 [9].
• DNA sequence analysis of regions from plasmid pIP417 and chromosome BF8 which encode 5-nitroimidazole resistance in Bacteroides strains allowed the identification of two open reading frames corresponding to new genes, nimA (528 bp) and nimB (492 bp) [2].

Chemical compound and disease context of NSC50359

• The complexes are compared with 4-nitroimidazole complexes of ruthenium, with respect to toxicity, binding and radiosensitization [10].
• Tinidazole is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa [11].
• Compound 21, with an arylsulfanyl group at C(5) of the 4-nitro-1H-imidazole backbone showed an EC(50) value of 0.22 mug/ml against HIV-1 with a therapeutic index of 13 [12].
• BACKGROUND: Giardia duodenalis is the most commonly detected parasite in the intestinal tract of humans and 5-nitroimidazole compounds, quinacrine and furazolidone have been used against giardiasis [13].

Biological context of NSC50359

• Nucleotide sequence analysis of two 5-nitroimidazole resistance determinants from Bacteroides strains and of a new insertion sequence upstream of the two genes [2].
• Genetics of resistance of Bacteroides species to 5-nitroimidazole [14].
• This pathway is responsible for metabolic activation of 5-nitroimidazole drugs, such as metronidazole, used in chemotherapy of trichomoniasis [15].
• Other incompletely elucidated aspects include mechanisms of pathogenicity, host reaction to infection, immunity and parasite control using vaccines or antigiardial compounds; the 5-nitroimidazole metronidazole is the most effective of these [16].
• Genetic analysis of the minimal replicon of plasmid pIP417 and comparison with the other encoding 5-nitroimidazole resistance plasmids from Bacteroides spp [17].

Anatomical context of NSC50359

• 5-Nitroimidazole derivative in the concentration of 300 micrograms/mg protein inhibited significantly the non-irradiated erythrocyte membrane (Na+, K+) ATP-ase activity, while 4-NO2 in the concentration of 3 micrograms/mg protein influenced this activity, but only after an exposure at dose of 60 Krad [18].
• Metronidazole, a 5-nitroimidazole drug has been reported to decrease testicular weight, testicular and epididymal spermatid counts and causes abnormal sperm morphology with degeneration of seminiferous tubules with 6 weeks treatment of metronidazole (400 mg/kg, day) [19].

Associations of NSC50359 with other chemical compounds

• Our data indicate that the 5-nitroimidazole CGI 17341 is a promising and novel antituberculosis compound with potent in vitro and in vivo activities [20].
• Secondly, Imuran, a 5-substituted 4-nitroimidazole and one of a series of compounds which show sensitizing efficiencies in vitro much greater than would be predicted from electron affinity considerations, also shows good sensitization in vivo [21].
• Cytotoxic properties of a 4-nitroimidazole (NSC 38087): a radiosensitizer of hypoxic cells in vitro [22].
• The water-soluble acetohydroxamates of 2-nitroimidazole (KIH-802; free acid 801) and 4-nitroimidazole (KIH-852) were designed, synthesized, and evaluated by in vitro and in vivo screening against EMT6 cells [23].
• Our results indicate that nifurtimox and related compounds act as redox cyclers, whereas the most active in the series, the 5-nitroimidazole megazol essentially acts as thiol scavenger particularly for trypanothione, the cofactor for trypanothione reductase, an essential enzyme in the detoxification process [24].

Gene context of NSC50359

• Identification and DNA sequence of the mobilization region of the 5-nitroimidazole resistance plasmid pIP421 from Bacteroides fragilis [25].
• Comparative efficacy of metronidazole and another 5-nitroimidazole, CG-10213-Go, in caecal amoebiasis in albino mice (Mus musculus) [26].
• 5-Nitroimidazole resistance assessed by the disc diffusion technique is not helpful in predicting OCT failure, but the E-test may be of value [27].
• We aimed to evaluate this using the disc diffusion technique (Mast Diagnostics, Bootle, UK) and E-test (Cambridge Diagnostics Services, Cambridge, UK) to assess 5-nitroimidazole resistance [27].
• The multiwavelength method may be used for samples degraded at pH 6-12 if the amount of conserved 5-nitroimidazole species is at least 93 mol.% of the original; the amounts of tinidazole and its two known impurities may be determined simultaneously [28].

Analytical, diagnostic and therapeutic context of NSC50359

• Detection by PCR of the nim genes encoding 5-nitroimidazole resistance in Bacteroides spp [29].
• Eleven of the labelled final reduction products of metronidazole (a 5-nitroimidazole) have been separated by high-performance liquid chromatography and identified [30].
• Thirty-three clinical isolates of Bacteroides strains with a moderate-to-high level of resistance to 5-nitroimidazole were compared with three strains previously studied by Southern blotting of their DNA [14].

References