• 미생물학회지
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• 제14권4호
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• pp.151-158
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• 1976

Using Ames'Salmonella/microsome system, mutagenicity of antirichomonal nitrofuran, nitroimidazole, and nitrothiazole derivatives was examined. Nitrofurantoin, nifuratel, furazolidone, metronidazole, nimorazole, ornidazole, and aminitrozole showed potent mutagenicity en $TA_100$ strain which is a base substitute mutant and contains R-factor plasmid pKM101 without microsomal enzyme activation. In addition, nifuratel, furazolidone, metronidazole, and ornidazole also induced frameshift mutation in $TA_98$ strain.

• 대한수의학회지
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• 제13권1호
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• pp.35-38
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• 1973

It was discovered that furamizole, one of the nitrofuran derivatives, possesses a strong antibacterial activity upon various organisms. Since then, a number of nitrofuran derivatives have been examined for antibacterial activity. This experiment was carried in vitro to evaluate with regard to antibacterial activity upon Mycoplasma gallisepticum. As a result, furamizole was found to be a good effective compound upon Mycoplasma gallisepticum. Furamizole inhibited the growths of the three strains of Mycoplasma gallisepticum and two strains of the same species at a concentration of $0.064{\mu}g/mI$. and $0.016{\mu}g/mI$. In short, there were not great differences in sensitivity to furamizole among the five strains tested.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.502-506
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• 2004

Two series of 2-(5-nitro-2-furyl)- and 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-propyl, allyl and propargyl)thio-1,3,4-thiadiazoles (6a-f) and 2-(5-nitro-2-furyl)- and 2-(1-methyl-5-nitro-1 H-imidazol-2-yl)-5-(nitrobenzyl)thio-1,3,4-thiadiazole derivatives (8a-f) have been synthesized and evaluated against Mycobacterium tuberculosis, as part of the TAACF TB screening program under direction of the US National Institute of Health, the NIAID division. Primary screening was conducted at a single concentration, 6.25 $\mu\textrm{g}$mL$^{-1}$ , against M. tuberculosis H$_{37}$ Rv in BACTEC 12B medium, using the Microplate Alamar Blue Assay (MABA). The minimum inhibitory concentration (MIC) was determined for the compounds that demonstrated $\geq$90% growth inhibition in the primary screening. A varying degree of antituberculosis activity (from 0-97% of growth inhibition) was observed with the alkylthio series (6a-f), and the nitroimidazole derivative with a propylthio group (6b) and the nitrofuran derivative with a propargylthio group (6e), were the most active compounds (MIC=3.13 and 1.56 /$\mu\textrm{g}$mL$^{-1}$ , respectively). Among the nitrobenzylthio derivatives (8a-f), all the ortho, meta and para nitrobenzyl isomers in the nitrofuran series exhibited good antituberculosis activity (MIC=3.13 $\mu\textrm{g}$mL$^{-1}$ ), while the corresponding nitroimidazole analogues were completely inactive (Inhibition=0%).

• 대한수의학회지
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• 제14권2호
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• pp.237-241
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• 1974

A number of chemotherapeutic agents, namely antibiotics, sulfonamides and nitrofuran derivatives have been used, as a fred additive, for the purposes of growth improvement of chicken, increase of feed efficiency, decrease of animal mortality, and disease prevention. In these experiments, furamizole which is one of nitrofuran derivatives and feed additive was test, in field, its antibacterial activity against Mycoplasma gallisepticum causing air sac disease, its effect on pullorum disease control, its effect on the lowering the mortality of chicken and finally the increase of feed efficiency. Throughout the studies, furamizole, in concentration of 0.025% in feed fed to baby chicken continuously resulted as following: 1. Tested chicken showed no avian mycoplasma infection compared to 3.7% outbreak in control chicken. 2. Tested chicken showed a low degree of outbreak of pullorum disease. However, its outbreak was much more surpresed compared to that of control chicken. 3. Total mortality rate of 5.5% and 30.8% were obtained in test and control chicken respectively. 4. Feed efficiency were 2.83 and 2.97 in test and control chicken respectively.

• 한국식품위생안전성학회지
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• 제31권2호
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• pp.85-93
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• 2016

미꾸라지에서의 Nitrofuran계 대사물질인3-amino-2-oxazolidone(AOZ), 5-morpholinomethyl-3-amino-2-oxazolidinone(AMOZ), 1-ammino-hydantoin (AHD)와 semicarbazide(SEM)의 잔류량을 검사하기 위해HPLC-MS/MS를 이용한 신속한 정량법이 개발되었다. 2-nitrobenzaldehyde (2-NBA)를 이용해 $50^{\circ}C$에서 1시간 동안 산 가수분해와 유도체화 과정을 거친 뒤에, 액-액 분배로 정제와 추출을 하였다. 회수율은 음성시료에 3가지 농도 0.5, 1.0, $2.0{\mu}g/kg$의 표준액을 첨가하여 평가하였고 평균 회수율은 75.1-108.1% 이었다. 정밀성(%RSD)은 일내 8.7% 이하, 일간 8.5% 이하였다. 직선성은 NBAOZ는 $0.2-20{\mu}g/Kg$, NBAMOZ는 $0.8-20{\mu}g/Kg$, NBAHD는 $0.2-20{\mu}g/Kg$, NBSEM 는 $0.1-20{\mu}g/Kg$ 범위에서 모두 상관계수 0.99이상이었다. 검출한계(LOD)는 NBAOZ $0.06{\mu}g/Kg$, NBAMOZ $0.24{\mu}g/Kg$, NBAHD $0.06{\mu}g/Kg$, NBSEM $0.03{\mu}g/Kg$이었고, 정량한계(LOQ)는 NBAOZ $0.2{\mu}g/Kg$, NBAMOZ $0.8{\mu}g/Kg$, NBAHD $0.2{\mu}g/Kg$, NBSEM $0.1{\mu}g/Kg$ 이었다. 가수분해 및 유도체화 소요시간을 1시간으로 줄여 만든 신속 간편한 이 시험법이 미꾸라지 중 nitrofuran metabolites잔류량 분석에 적합함을 확인할 수 있었다.

• 약학회지
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• 제21권4호
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• pp.184-192
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• 1977

In the presence of dithionite, two kinds of molybdothiol complexes, particularly isolated Mo-cysteine complexes, used as models for xanthine oxidase or aldehyde oxidase exhibited catalytic activity on the reduction of nitrofurazone to its amino derivative. Of the two Mo-cysteine complexes, the activity of oxo-bridged one was apparently greater than that of sulfido-bridged one. The promoting effect was hardly shown by added cofactors or their replacements of the enzymes. The catalyzed reduction is considered to take place by consecutive direct two-electron transfer mechanism from catalytically active reduced form of the molybdothiol complexes to nitrofurazone and the probable intermediates.

• 한국식품위생안전성학회지
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• 제7권2호
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• pp.107.2-119
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• 1992

Fish pathology is one of the main scientific bases upon which this expansion in aquaculture has been dependent and requires a wide knowledge of the environmental constraints, the physiology and characteristic of the various pathogens, the responses of the host, and the methods by which they may be controlled. The primary disease and parasite problems in aquaculture animals related to viral, bacteria, fungal and protozoan epizootics. Parasitic nematodes, trematodes and cestodes are commonly found in aquaculture animals, but seldom are they present in concentrations sufficient to cause significant problems, When an epizootic does occur and chemical treatment is indicated, the appropriate chemical must be selected an properly applied. We have antibiotics, sulfa, nitrofuran and other chemicals for treatment of fish diseases, Some may be mixed with the feed during formulation, added to the pellets of feed as a surface coating, given in the form of an injection or used as a bath. Even though a drug or chemical has been officially approved for use in aquaculture, the substance should never be used unless there is a clear need, Some of the reasions for this view are as follows: (1) the constant use of antibiotics can leak to the development of resistant strains of bacteria, (2) biofilter efficiency may be impaired or destroyed by chemicals added to closed recirculating water systems, and(3) the injudicious use of chemical can have a damaging effect on the environment as well as on human.

• Parasites, Hosts and Diseases
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• 제54권2호
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• pp.155-161
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• 2016

Toxoplasma gondii is an important opportunistic pathogen that causes toxoplasmosis, which has very few therapeutic treatment options. The most effective therapy is a combination of pyrimethamine and sulfadiazine; however, their utility is limited because of drug toxicity and serious side effects. For these reasons, new drugs with lower toxicity are urgently needed. In this study, the compound, (Z)-1-[(5-nitrofuran-2-yl)methyleneamino]-imidazolidine-2,4-dione (nitrofurantoin), showed anti-T. gondii effects in vitro and in vivo. In HeLa cells, the selectivity of nitrofurantoin was 2.3, which was greater than that of pyrimethamine (0.9). In T. gondii-infected female ICR mice, the inhibition rate of T. gondii growth in the peritoneal cavity was 44.7% compared to the negative control group after 4-day treatment with 100 mg/kg of nitrofurantoin. In addition, hematology indicators showed that T. gondii infection-induced serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels, biochemical parameters involved in liver injury, were reduced by nitrofurantoin significantly. Moreover, nitrofurantoin exerted significant effects on the index of antioxidant status, i.e., malondialdehyde (MDA) and glutathione (GSH). The nitrofurantoin-treated group inhibited the T. gondii-induced MDA levels while alleviating the decrease in GSH levels. Thus, nitrofurantoin is a potential anti-T. gondii candidate for clinical application.

• 한국식품위생안전성학회:학술대회논문집
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• 한국식품위생안전성학회 1992년도 학술강연회
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• pp.7-19
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• 1992

Fish pathology is one of the main scientific bases upon which this expansion in aquaculture has been dependent and requires a wide knowledge of the environmental constraints, the physiology and characteristics of the various pathogens, the responses of the host and the methods by which they may be controlled. The primary disease and parasite problems in aquaculture animals relate to viral, bacterial, fungal and protozoan epizootics. Parasitic nematodes, trematodes and cestodes are commonly found in aquaculture animals, but seldom are they present in concentrations sufficinet to cause significant problems. When an epizootic does occur and chemical treatment is indicated, the appropriate chemical must be selected and properly applied. We have antibiotics, sulfa, nitrofuran and other chemicals for treatment of fish diseases. Some may be mixed with the fred during formulation, added to the pellets of feed as a surface coating, given in the dorm of an injection or used as a bath. Even though a drug or chemical has been officially approved for use in aquaculture, the substance should never be used unless there is a clear need. Some of the reasions for this view are as follows: (1) the constant use of antibiotics can lead to the development of resistant strains of bacteria, (2) biofilter efficiency may be impaired or destroyed by chemicals added to closed recirculating water systems, and (3) the injudicious use of chemicals can have a damaging effect on the environment as well as on human.

• 생약학회지
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• 제40권2호
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• pp.137-142
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• 2009

Isoniazid was discovered in 1950's and since then it has been widely used as a synthetic bactericidal agent in the treatment of tuberculosis. However, the adverse effect of isoniazid has been reported to show significant hepatotoxicity in approximately 1-2% of patients. Nitrofurantoin {1-(5-nitro-2-furfurylideneamino)-hydantoin} is a synthetic nitrofuran that is commonly used for the treatment and prophylaxis of urinary tract infections, but its use is associated with liver cirrhosis and fatal liver necrosis. Therefore, studies for natural products with protective effect on the isoniazid- and/or nitrofurantoin-induced hepatotoxcity would be valuable as the potential therapeutic use. 107 plants sources were collected at Mt. Baekdu, and extracted with methanol. These extracts had been screened for the protective effects against isoniazid- and/or nitrofurantoin-induced cytotoxicity in HepG2 cells at the both 100 and $300{\mu}g/ml$. Five methanolic extracts, Acanthopanax senticosus, Acer mono, Asparagus schoberioides, Fagopyrum tataricum, Potentilla centigrana, showed significant protective effects against isoniazidinduced hepatotoxicity. Two methanolic extracts, Acer mono and Leonurus artemisia, showed significant protective effects against nitrofurantoin-induced cytotoxicity in HepG2 cells.