Nitroimidazoles are a class of antibacterial and antiprotozoal drugs, which, upon reduction, interact with bacterial or protozoal DNA leading to inhibition of nucleic acid synthesis and ultimately cell death, used primarily in the treatment of anaerobic infections and certain parasitic diseases.
A nitroimidazole that sensitizes normally radio-resistant hypoxic cells to radiation. It may also be directly cytotoxic to hypoxic cells and has been proposed as an antineoplastic.
A genus of flagellate EUKARYOTES possessing three long anterior flagella.
Enzymes which reduce nitro groups (NITRO COMPOUNDS) and other nitrogenous compounds.
Nitrofurans are a group of synthetic antibacterial agents, characterized by a nitrofuran moiety, that exhibit broad-spectrum antimicrobial activity, primarily targeting gram-positive and gram-negative bacteria in the urinary tract, and are used mainly for the treatment and prevention of lower urinary tract infections.
Agents used to treat trichomonas infections.
A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS. It has also been proposed as a radiation sensitizer for hypoxic cells. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985, p133), this substance may reasonably be anticipated to be a carcinogen (Merck, 11th ed).
A nitroimidazole that sensitizes hypoxic tumor cells that are normally resistant to radiation therapy.
A species of TRICHOMONAS that produces a refractory vaginal discharge in females, as well as bladder and urethral infections in males.
A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.
Drugs used to potentiate the effectiveness of radiation therapy in destroying unwanted cells.
Drugs used to treat or prevent parasitic infections.
Six-membered heterocycles containing an oxygen and a nitrogen.
A nitroimidazole antitrichomonal agent effective against Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia infections.
Life or metabolic reactions occurring in an environment containing oxygen.
The complete absence, or (loosely) the paucity, of gaseous or dissolved elemental oxygen in a given place or environment. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
Drugs used in the treatment of tuberculosis. They are divided into two main classes: "first-line" agents, those with the greatest efficacy and acceptable degrees of toxicity used successfully in the great majority of cases; and "second-line" drugs used in drug-resistant cases or those in which some other patient-related condition has compromised the effectiveness of primary therapy.
Inbred C3H mice are a strain of laboratory mice that have been selectively bred to maintain a high degree of genetic uniformity and share specific genetic characteristics, including susceptibility to certain diseases, which makes them valuable for biomedical research purposes.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)

Evidence of hypoxic areas within the arterial wall in vivo. (1/721)

The anoxemia theory of atherosclerosis states that an imbalance between the demand and supply of oxygen in the arterial wall is a key factor for the development of atherosclerotic lesions. Direct in vitro and in situ measurements have shown that PO2 is decreased in the more deeply situated parts of the media, but the degree of hypoxia in vivo or the distribution of hypoxia along the arterial tree is not known. For this reason, we have developed a method for the detection of hypoxia in the arterial wall in vivo by using a hypoxia marker, 7-(4'-(2-nitroimidazol-1-yl)-butyl)-theophylline, that may be visualized by immunofluorescence. In the present study, we have used this method in rabbits with experimentally induced atherosclerosis. Our results indicate that zones of hypoxia occur at depth in the atherosclerotic plaque. The mechanism was probably an impaired oxygen diffusion capacity due to the thickness of the lesion, together with high oxygen consumption by the foam cells. Thus, we have for the first time demonstrated that hypoxia actually does exist in the arterial wall in vivo, lending support to the anoxemia theory of atherosclerosis.  (+info)

A bioluminescence method for the mapping of local ATP concentrations within the arterial wall, with potential to assess the in vivo situation. (2/721)

According to the anoxemia theory of atherosclerosis, an imbalance between the demand for and supply of oxygen and nutrients in the arterial wall is a key factor in atherogenesis. However, the energy metabolic state of the arterial tissue in vivo is largely unknown. We applied a bioluminescence method, metabolic imaging, to study local ATP concentrations in cryosections of normal pig and atherosclerotic and normal rabbit aorta. Some vessels were subjected to energy metabolic restrictions by incubation at different oxygen and glucose concentrations and others were rapidly frozen in liquid nitrogen to reflect the in vivo situation. Local ATP concentrations and the ATP distribution at a microscale was dependent on oxygen as well as glucose concentrations during incubation. ATP depletion was seen in the mid media of pig aorta in all incubations, but only at low oxygen concentration without glucose in the media of the thinner rabbit aorta. ATP-depleted zones were seen deep in pig media (>750 microm from the lumen) and in rabbit plaques (>300 micrometer+ from the lumen) even at high oxygen (pig 75% O2 and rabbit 21% O2) and glucose concentrations (5.6 mmol/L glucose). This observation probably illustrates an insufficient diffusion of glucose, which highlights the importance of studying the conditions for diffusion not only of oxygen but also of other metabolites in the arterial wall. In rapidly frozen vessels the medial ATP concentration was shown to be 0.6 to 0.8 micromol/g wet weight (both pig and rabbit aorta) and in pig aorta a gradient could be seen indicating higher ATP concentrations at the lumenal side. We propose that metabolic imaging, as applied to snap-frozen tissue, may be used to assess the energy metabolic situation in the arterial wall in vivo. The spatial resolution allows the detection of local variations within the arterial tree. However, steep concentration gradients (eg, near the border of the tissue) will be underestimated. The method may be extended to include determinations of glucose and lactate concentrations and will be used in parallel with an established method to assess hypoxia in the arterial wall in vivo.  (+info)

Reperfusion injury in livers due to gentle in situ organ manipulation during harvest involves hypoxia and free radicals. (3/721)

Kupffer cell-dependent injury in livers gently manipulated during harvest develops upon transplantation; however, underlying mechanisms remain unknown. Thus, the purpose of this study was to identify factors involved in mechanisms of injury. Livers from female Sprague-Dawley rats (200-230 g) were cold stored for 24 h in University of Wisconsin solution. Subsequently, livers were perfused at 37 degrees C with oxygen-saturated Krebs-Henseleit buffer containing fluorescein-dextran to assess microcirculation. Cell death was assessed by uptake of trypan blue, a vital dye. Minimal dissection during harvest had no effects on sinusoidal lining cells; however, gentle organ manipulation dramatically increased trypan blue uptake about 5-fold (p <.05). In contrast, perfusion with N2-saturated buffer after cold storage totally prevented cell death due to manipulation. At harvest, portal venous pressure was increased significantly by 70% due to manipulation. Furthermore, vascular space and microcirculation were decreased by more than 50% (p <.05), reflecting the rate of entry and exit of fluorescein-dextran. Pimonidazole, a 2-nitroimidazole marker, was given to rats before harvest to detect hypoxia in liver. Pimonidazole adduct binding was increased significantly about 2-fold by manipulation. To detect free radical adducts by electron spin resonance (ESR) spectroscopy in bile, C-phenyl-N-tert-butylnitrone was given as spin trapping reagent to the donor before operation. Free radical formation was increased about 3-fold by organ manipulation (p <.05). Donors given gadolinium chloride, a selective Kupffer cell toxicant, or dietary glycine, which prevents activation of Kupffer cells, significantly blunted microcirculatory disturbances, hypoxia, and death of endothelial lining cells. These data indicate for the first time that gentle organ manipulation during harvest causes oxygen-dependent reperfusion injury to endothelial lining cells via mechanisms involving hepatic microcirculation, hypoxia, and Kupffer cells.  (+info)

Hepatocellular hypoxia-induced vascular endothelial growth factor expression and angiogenesis in experimental biliary cirrhosis. (4/721)

We tested the potential role of vascular endothelial growth factor (VEGF) and of fibroblast growth factor-2 (FGF-2) in the angiogenesis associated with experimental liver fibrogenesis induced by common bile duct ligation in Sprague-Dawley rats. In normal rats, VEGF and FGF-2 immunoreactivities were restricted to less than 3% of hepatocytes. One week after bile duct ligation, hypoxia was demonstrated by the immunodetection of pimonidazole adducts unevenly distributed throughout the lobule. After 2 weeks, hypoxia and VEGF expression were detected in >95% of hepatocytes and coexisted with an increase in periportal vascular endothelial cell proliferation, as ascertained by Ki67 immunolabeling. Subsequently, at 3 weeks the density of von Willebrand-labeled vascular section in fibrotic areas significantly increased. Semiquantitative reverse transcription polymerase chain reaction showed that VEGF(120) and VEGF(164) transcripts, that correspond to secreted isoforms, increased within 2 weeks, while VEGF(188) transcripts remained unchanged. FGF-2 mainly consisting of a 22-kd isoform, according to Western blot, was identified by immunohistochemistry in 49% and 100% of hepatocytes at 3 and 7 weeks, respectively. Our data provide evidence that in biliary-type liver fibrogenesis, angiogenesis is stimulated primarily by VEGF in response to hepatocellular hypoxia while FGF-2 likely contributes to the maintenance of angiogenesis at later stages.  (+info)

Benznidazole, a drug employed in the treatment of Chagas' disease, down-regulates the synthesis of nitrite and cytokines by murine stimulated macrophages. (5/721)

Benznidazole (BZL) is a nitroheterocyclic drug employed in the chemotherapy of Chagas' disease, a protozoan disease caused by Trypanosoma cruzi. Because this parasite mostly replicates in macrophages, we investigated whether BZL was likely to modify the synthesis of macrophage mediators such as nitrite, tumour necrosis factor-alpha (TNF-alpha), IL-1beta, IL-6 and IL-10. Control and stimulated murine macrophages (lipopolysaccharide (LPS) and/or interferon-gamma (IFN-gamma)) were treated with BZL and measurements were carried out in culture supernatants collected 24 h later. Synthesis of nitrite, IL-6 and IL-10 was maximal upon combined stimulation with LPS + IFN-gamma, whereas lower amounts of the three mediators were detected when both stimuli were given alone. BZL treatment significantly reduced nitrite, IL-6 and IL-10 production, to undetectable levels in some cases, particularly IL-6 and IL-10. LPS was the most potent stimulus of IL-1beta and TNF-alpha production, followed by LPS + IFN-gamma and IFN-gamma in decreasing order. BZL partly inhibited TNF-alpha synthesis, but this effect was smaller than that observed for nitrite, IL-6 and IL-10. LPS-induced production of IL-1beta was also affected by BZL. Semiquantification of gene expression for inducible nitric oxide synthase (iNOS) showed that BZL completely inhibited iNOS gene induction by IFN-gamma, and resulted in respective inhibitions of 30% and 50% with LPS- and LPS + IFN-gamma-stimulated cells. BZL was not cytotoxic on macrophage cultures, as shown by the lactate dehydrogenase activity. Besides its trypanocidal activity, BZL may also alter the balance between pro- and anti-inflammatory mediators with important consequences for the course of T. cruzi infection.  (+info)

Improved fidelity of thermostable ligases for detection of microsatellite repeat sequences using nucleoside analogs. (6/721)

Microsatellite repeats consisting of dinucleotide sequences are ubiquitous in the human genome and have proven useful for linkage analysis, positional cloning and forensic identification purposes. In this study, the potential of utilizing the ligase detection reaction for the analysis of such microsatellite repeat sequences was investigated. Initially, the fidelity of thermostable DNA ligases was measured for model dinucleotide repeat sequences. Subsequently, the effect of modified oligonucleotides on ligation fidelity for dinucleotide repeats was determined using the nucleoside analogs nitroimidazole, inosine, 7-deazaguanosine and 2-pyrimidinone, as well as natural base mismatches. The measured error rates for a standard dinucleotide template indicated that the nitroimidazole nucleoside analogs could be used to increase the fidelity of ligation when compared to unmodified primers. Furthermore, use of formamide in the ligation buffer also increased ligation fidelity for dinucleotide repeat sequences. Using ligation-based assays to detect polymorphic alleles of microsatellite repeats in the human genome opens the possibility of using array-based typing of these loci for human identification, loss-of-heterozygosity studies and linkage analysis.  (+info)

Soluble platelet selectin (sP-selectin) and soluble vascular cell adhesion molecule-1 (sVCAM-1) decrease during therapy with benznidazole in children with indeterminate form of Chagas' disease. (7/721)

The immune response against Trypanosoma cruzi infection has been associated with both protection and pathogenesis. Central events in host defence system- and immune-mediated damage are tightly regulated by cell adhesion molecules (CAM). Levels of sP-selectin and sVCAM-1 were measured in sera from 41 children with the indeterminate phase of Chagas' disease. Simultaneously, levels of soluble adhesion molecule were also quantified in Chagas' disease children undergoing specific chemotherapy with benznidazole. Levels of sP-selectin and sVCAM-1 were found to be elevated in children with indeterminate Chagas' disease before aetiologic therapy was started. However, a small group of patients showed sP-selectin and sVCAM-1 levels comparable to those of non-infected children. A positive correlation between levels of sVCAM-1 and sP-selectin in sera from Chagas' disease patients was found. There was a significantly greater decrease in the titres of sP-selectin and sVCAM-1 in those children receiving benznidazole therapy compared with those children receiving placebo. Measurement of soluble adhesion molecules revealed differences in the activation of the immune system in children with the indeterminate form of Chagas' disease. The early decrease of sP-selectin and sVCAM-1 levels after anti-parasitic treatment suggests that these molecules might be valuable indicators of effective parasitologic clearance.  (+info)

Activities of the triazole derivative SCH 56592 (posaconazole) against drug-resistant strains of the protozoan parasite Trypanosoma (Schizotrypanum) cruzi in immunocompetent and immunosuppressed murine hosts. (8/721)

We have studied the in vivo activity of the new experimental triazole derivative SCH 56592 (posaconazole) against a variety of strains of the protozoan parasite Trypanosoma (Schizotrypanum) cruzi, the causative agent of Chagas' disease, in both immunocompetent and immunosuppressed murine hosts. The T. cruzi strains used in the study were previously characterized as susceptible (CL), partially resistant (Y), or highly resistant (Colombiana, SC-28, and VL-10) to the drugs currently in clinical use, nifurtimox and benznidazole. Furthermore, all strains are completely resistant to conventional antifungal azoles, such as ketoconazole. In the first study, acute infections with the CL, Y, and Colombiana strains in both normal and cyclophosphamide-immunosuppressed mice were treated orally, starting 4 days postinfection (p.i.), for 20 consecutive daily doses. The results indicated that in immunocompetent animals SCH 56592 at 20 mg/kg of body weight/day provided protection (80 to 90%) against death caused by all strains, a level comparable or superior to that provided by the optimal dose of benznidazole (100 mg/kg/day). Evaluation of parasitological cure revealed that SCH 56592 was able to cure 90 to 100% of the surviving animals infected with the CL and Y strains and 50% of those which received the benznidazole- and nifurtimox-resistant Colombiana strain. Immunosuppression markedly reduced the mean survival time of untreated mice infected with any of the strains, but this was not observed for the groups which received SCH 56592 at 20 mg/kg/day or benznidazole at 100 mg/kg/day. However, the overall cure rates were higher for animals treated with SCH 56592 than among those treated with benznidazole. The results were confirmed in a second study, using the same model but a longer (43-dose) treatment period. Finally, a model for the chronic disease in which oral treatment was started 120 days p.i. and consisted of 20 daily consecutive doses was investigated. The results showed that SCH 56592 at 20 mg/kg/day was able to induce a statistically significant increase in survival of animals infected with all strains, while benznidazole at 100 mg/kg/day was able to increase survival only in animals infected with the Colombiana strain. Moreover, the triazole was able to induce parasitological cures in 50 to 60% of surviving animals, irrespective of the infecting strain, while no cures were obtained with benznidazole. Taken together, the results demonstrate that SCH 56592 has in vivo trypanocidal activity, even against T. cruzi strains naturally resistant to nitrofurans, nitroimidazoles, and conventional antifungal azoles, and that this activity is retained to a large extent in immunosuppressed hosts.  (+info)

Nitroimidazoles are a class of antibiotic drugs that contain a nitro group (-NO2) attached to an imidazole ring. These medications have both antiprotozoal and antibacterial properties, making them effective against a range of anaerobic organisms, including bacteria and parasites. They work by being reduced within the organism, which leads to the formation of toxic radicals that interfere with DNA function and ultimately kill the microorganism.

Some common examples of nitroimidazoles include:

* Metronidazole: used for treating infections caused by anaerobic bacteria and protozoa, such as bacterial vaginosis, amebiasis, giardiasis, and pseudomembranous colitis.
* Tinidazole: similar to metronidazole, it is used to treat various infections caused by anaerobic bacteria and protozoa, including trichomoniasis, giardiasis, and amebiasis.
* Secnidazole: another medication in this class, used for the treatment of bacterial vaginosis, trichomoniasis, and amebiasis.

Nitroimidazoles are generally well-tolerated, but side effects can include gastrointestinal symptoms like nausea, vomiting, or diarrhea. Rare but serious side effects may include peripheral neuropathy (nerve damage) and central nervous system toxicity, particularly with high doses or long-term use. It is essential to follow the prescribed dosage and duration closely to minimize potential risks while ensuring effective treatment.

Misonidazole is defined as a radiosensitizer drug, which is primarily used in the field of radiation oncology. It works by making cancer cells more sensitive to radiation therapy, thereby increasing the effectiveness of the treatment. Misonidazole is an nitroimidazole compound that gets reduced under hypoxic conditions (when there is a lack of oxygen) and forms free radicals, which can damage DNA and kill the cells.

It's important to note that misonidazole is not commonly used in current clinical practice due to its narrow therapeutic index and significant side effects, such as neurotoxicity. Other nitroimidazole radiosensitizers, such as nimorazole, have been developed and are more widely used because they have a lower risk of neurotoxicity.

Tritrichomonas is a genus of protozoan parasites that are commonly found in the digestive tracts of various animals, including humans. The most well-known species is Tritrichomonas foetus, which is a significant pathogen in cattle, causing a venereal disease known as bovine trichomoniasis.

In humans, Tritrichomonas vaginalis is the species that is associated with infection, specifically in the urogenital tract of women. It can cause a condition called trichomoniasis, which is typically characterized by vaginitis (inflammation of the vagina) and discharge. However, it's important to note that many people infected with T. vaginalis are asymptomatic, and the infection can sometimes lead to more severe complications such as preterm labor or premature rupture of membranes during pregnancy.

Tritrichomonas species are characterized by having three flagella at the anterior end and one at the posterior end, which they use for movement. They are usually transmitted through direct contact with infected individuals or contaminated fomites. Proper diagnosis and treatment are essential to prevent the spread of infection and potential complications.

Nitroreductases are a group of enzymes that can reduce nitro groups (-NO2) to nitroso groups (-NHOH) or amino groups (-NH2) in various organic compounds. These enzymes are widely distributed in nature and found in many different types of organisms, including bacteria, fungi, plants, and animals.

In medicine, nitroreductases have been studied for their potential role in the activation of certain drugs or prodrugs. For example, some anticancer agents such as CB1954 (also known as 5-(aziridin-1-yl)-2,4-dinitrobenzamide) are relatively inert until they are reduced by nitroreductases to more reactive metabolites that can interact with DNA and other cellular components. This property has been exploited in the development of targeted cancer therapies that selectively deliver prodrugs to tumor cells, where they can be activated by endogenous nitroreductases to kill the cancer cells while minimizing toxicity to normal tissues.

Nitroreductases have also been implicated in the development of bacterial resistance to certain antibiotics, such as metronidazole and nitrofurantoin. These drugs are activated by nitroreductases in bacteria, but overexpression or mutation of the enzyme can lead to reduced drug activation and increased resistance.

Nitrofurans are a group of synthetic antibacterial agents that have been widely used in the medical field for their antimicrobial properties. The primary use of nitrofurans is to treat urinary tract infections (UTIs) caused by susceptible strains of bacteria. Nitrofurantoin is the most commonly prescribed nitrofuran and is available under various brand names, such as Macrobid and Furadantin.

Nitrofurans have a unique mechanism of action that distinguishes them from other antibiotics. They require an aerobic environment with an adequate concentration of oxygen to be effective. Once inside the body, nitrofurans are rapidly metabolized and concentrated in urine, where they exhibit bactericidal activity against various gram-positive and gram-negative bacteria, including Escherichia coli, Staphylococcus saprophyticus, and Enterococci.

The antibacterial action of nitrofurans is attributed to their ability to inhibit essential bacterial enzymes involved in nucleic acid synthesis, energy production, and cell wall biosynthesis. This multifaceted mechanism of action makes it difficult for bacteria to develop resistance against nitrofurans.

Common side effects associated with nitrofurantoin include gastrointestinal symptoms such as nausea, vomiting, and diarrhea. Less frequently, patients may experience headaches, dizziness, or skin rashes. In rare cases, nitrofurantoin can cause pulmonary reactions, hepatotoxicity, or peripheral neuropathy.

Due to the potential for adverse effects and the risk of developing drug-resistant bacteria, nitrofurans should only be prescribed when there is a strong clinical indication and susceptibility testing has been performed. Patients with impaired renal function, pregnant women in their third trimester, or those with a history of liver or lung disease may not be suitable candidates for nitrofuran therapy due to the increased risk of adverse reactions.

Antitrichomonatal agents are a group of medications specifically used to treat infections caused by the protozoan parasite, Trichomonas vaginalis. The most common antitrichomonal agent is metronidazole, which works by disrupting the parasite's ability to reproduce and survive within the human body. Other antitrichomonal agents include tinidazole and secnidazole, which also belong to the nitroimidazole class of antibiotics. These medications are available in various forms, such as tablets, capsules, or topical creams, and are typically prescribed by healthcare professionals for the treatment of trichomoniasis, a common sexually transmitted infection (STI) that can affect both men and women. It is important to note that these medications should only be used under the guidance of a healthcare provider, as they may have potential side effects and drug interactions.

Metronidazole is an antibiotic and antiprotozoal medication. It is primarily used to treat infections caused by anaerobic bacteria and certain parasites. Metronidazole works by interfering with the DNA of these organisms, which inhibits their ability to grow and multiply.

It is available in various forms, including tablets, capsules, creams, and gels, and is often used to treat conditions such as bacterial vaginosis, pelvic inflammatory disease, amebiasis, giardiasis, and pseudomembranous colitis.

Like all antibiotics, metronidazole should be taken only under the direction of a healthcare provider, as misuse can lead to antibiotic resistance and other complications.

Etanidazole is an antitumor agent, specifically a nitroimidazole radioprotector and radiosensitizer. It works by reducing the amount of oxygen that is needed for radiation to damage tumor cells, making the radiation therapy more effective. Etanidazole is used in the treatment of brain tumors and other solid tumors, often in combination with radiation therapy.

The medical definition of 'Etanidazole' is:

A nitroimidazole antitumor agent that is a radioprotector and radiosensitizer, increasing the effectiveness of radiation therapy in the treatment of brain tumors and other solid tumors. It works by reducing the amount of oxygen needed for radiation to damage tumor cells.

Trichomonas vaginalis is a species of protozoan parasite that causes the sexually transmitted infection known as trichomoniasis. It primarily infects the urogenital tract, with women being more frequently affected than men. The parasite exists as a motile, pear-shaped trophozoite, measuring about 10-20 micrometers in size.

T. vaginalis infection can lead to various symptoms, including vaginal discharge with an unpleasant odor, itching, and irritation in women, while men may experience urethral discharge or discomfort during urination. However, up to 50% of infected individuals might not develop any noticeable symptoms, making the infection challenging to recognize and treat without medical testing.

Diagnosis typically involves microscopic examination of vaginal secretions or urine samples, although nucleic acid amplification tests (NAATs) are becoming more common due to their higher sensitivity and specificity. Treatment usually consists of oral metronidazole or tinidazole, which are antibiotics that target the parasite's ability to reproduce. It is essential to treat both partners simultaneously to prevent reinfection and ensure successful eradication of the parasite.

Ornidazole is an antiprotozoal and antibacterial medication. It is primarily used to treat infections caused by susceptible anaerobic bacteria and protozoan parasites. Ornidazole works by disrupting the DNA of these microorganisms, leading to their death.

Common indications for its use include the treatment of various types of bacterial infections such as skin and soft tissue infections, bone and joint infections, intra-abdominal infections, and gynecological infections. It is also used to treat certain protozoan infections, including amebiasis and giardiasis.

Ornidazole is available in various forms, such as tablets, capsules, and intravenous (IV) solutions, and its use should be based on the specific infection being treated and the patient's individual medical history. As with any medication, it can have side effects, and its use should be monitored by a healthcare professional to ensure its safe and effective use.

Radiation-sensitizing agents are drugs that make cancer cells more sensitive to radiation therapy. These agents work by increasing the ability of radiation to damage the DNA of cancer cells, which can lead to more effective tumor cell death. This means that lower doses of radiation may be required to achieve the same therapeutic effect, reducing the potential for damage to normal tissues surrounding the tumor.

Radiation-sensitizing agents are often used in conjunction with radiation therapy to improve treatment outcomes for patients with various types of cancer. They can be given either systemically (through the bloodstream) or locally (directly to the tumor site). The choice of agent and the timing of administration depend on several factors, including the type and stage of cancer, the patient's overall health, and the specific radiation therapy protocol being used.

It is important to note that while radiation-sensitizing agents can enhance the effectiveness of radiation therapy, they may also increase the risk of side effects. Therefore, careful monitoring and management of potential toxicities are essential during treatment.

Antiparasitic agents are a type of medication used to treat parasitic infections. These agents include a wide range of drugs that work to destroy, inhibit the growth of, or otherwise eliminate parasites from the body. Parasites are organisms that live on or inside a host and derive nutrients at the host's expense.

Antiparasitic agents can be divided into several categories based on the type of parasite they target. Some examples include:

* Antimalarial agents: These drugs are used to treat and prevent malaria, which is caused by a parasite that is transmitted through the bites of infected mosquitoes.
* Antiprotozoal agents: These drugs are used to treat infections caused by protozoa, which are single-celled organisms that can cause diseases such as giardiasis, amoebic dysentery, and sleeping sickness.
* Antihelminthic agents: These drugs are used to treat infections caused by helminths, which are parasitic worms that can infect various organs of the body, including the intestines, lungs, and skin. Examples include roundworms, tapeworms, and flukes.

Antiparasitic agents work in different ways to target parasites. Some disrupt the parasite's metabolism or interfere with its ability to reproduce. Others damage the parasite's membrane or exoskeleton, leading to its death. The specific mechanism of action depends on the type of antiparasitic agent and the parasite it is targeting.

It is important to note that while antiparasitic agents can be effective in treating parasitic infections, they can also have side effects and potential risks. Therefore, it is essential to consult with a healthcare provider before starting any antiparasitic medication to ensure safe and appropriate use.

Oxazines are heterocyclic organic compounds that contain a six-membered ring with one nitrogen atom, one oxygen atom, and four carbon atoms. The structure of oxazine is similar to benzene, but with one methine group (=CH−) replaced by a nitrogen atom and another methine group replaced by an oxygen atom.

Oxazines have important applications in the pharmaceutical industry as they are used in the synthesis of various drugs, including anti-inflammatory, antiviral, and anticancer agents. However, oxazines themselves do not have a specific medical definition, as they refer to a class of chemical compounds rather than a medical condition or treatment.

Tinidazole is an antiprotozoal and antibacterial medication used to treat various infections caused by parasites or bacteria. According to the Medical Dictionary, it is defined as:

"A synthetic nitroimidazole antimicrobial agent, similar to metronidazole, that is active against a wide range of anaerobic bacteria and protozoa, both pathogenic and nonpathogenic. It is used in the treatment of various clinical conditions, including bacterial vaginosis, amebiasis, giardiasis, trichomoniasis, and pseudomembranous colitis."

Tinidazole works by interfering with the DNA of the microorganisms, which leads to their death. It is available in oral tablet form and is typically prescribed for a duration of 2-5 days, depending on the type and severity of the infection being treated. Common side effects may include nausea, vomiting, diarrhea, stomach pain, headache, and changes in taste sensation.

Aerobiosis is the process of living, growing, and functioning in the presence of oxygen. It refers to the metabolic processes that require oxygen to break down nutrients and produce energy in cells. This is in contrast to anaerobiosis, which is the ability to live and grow in the absence of oxygen.

In medical terms, aerobiosis is often used to describe the growth of microorganisms, such as bacteria and fungi, that require oxygen to survive and multiply. These organisms are called aerobic organisms, and they play an important role in many biological processes, including decomposition and waste breakdown.

However, some microorganisms are unable to grow in the presence of oxygen and are instead restricted to environments where oxygen is absent or limited. These organisms are called anaerobic organisms, and their growth and metabolism are referred to as anaerobiosis.

Anaerobiosis is a state in which an organism or a portion of an organism is able to live and grow in the absence of molecular oxygen (O2). In biological contexts, "anaerobe" refers to any organism that does not require oxygen for growth, and "aerobe" refers to an organism that does require oxygen for growth.

There are two types of anaerobes: obligate anaerobes, which cannot tolerate the presence of oxygen and will die if exposed to it; and facultative anaerobes, which can grow with or without oxygen but prefer to grow in its absence. Some organisms are able to switch between aerobic and anaerobic metabolism depending on the availability of oxygen, a process known as "facultative anaerobiosis."

Anaerobic respiration is a type of metabolic process that occurs in the absence of molecular oxygen. In this process, organisms use alternative electron acceptors other than oxygen to generate energy through the transfer of electrons during cellular respiration. Examples of alternative electron acceptors include nitrate, sulfate, and carbon dioxide.

Anaerobic metabolism is less efficient than aerobic metabolism in terms of energy production, but it allows organisms to survive in environments where oxygen is not available or is toxic. Anaerobic bacteria are important decomposers in many ecosystems, breaking down organic matter and releasing nutrients back into the environment. In the human body, anaerobic bacteria can cause infections and other health problems if they proliferate in areas with low oxygen levels, such as the mouth, intestines, or deep tissue wounds.

Antitubercular agents, also known as anti-tuberculosis drugs or simply TB drugs, are a category of medications specifically used for the treatment and prevention of tuberculosis (TB), a bacterial infection caused by Mycobacterium tuberculosis. These drugs target various stages of the bacteria's growth and replication process to eradicate it from the body or prevent its spread.

There are several first-line antitubercular agents, including:

1. Isoniazid (INH): This is a bactericidal drug that inhibits the synthesis of mycolic acids, essential components of the mycobacterial cell wall. It is primarily active against actively growing bacilli.
2. Rifampin (RIF) or Rifampicin: A bactericidal drug that inhibits DNA-dependent RNA polymerase, preventing the transcription of genetic information into mRNA. This results in the interruption of protein synthesis and ultimately leads to the death of the bacteria.
3. Ethambutol (EMB): A bacteriostatic drug that inhibits the arabinosyl transferase enzyme, which is responsible for the synthesis of arabinan, a crucial component of the mycobacterial cell wall. It is primarily active against actively growing bacilli.
4. Pyrazinamide (PZA): A bactericidal drug that inhibits the synthesis of fatty acids and mycolic acids in the mycobacterial cell wall, particularly under acidic conditions. PZA is most effective during the initial phase of treatment when the bacteria are in a dormant or slow-growing state.

These first-line antitubercular agents are often used together in a combination therapy to ensure complete eradication of the bacteria and prevent the development of drug-resistant strains. Treatment duration typically lasts for at least six months, with the initial phase consisting of daily doses of INH, RIF, EMB, and PZA for two months, followed by a continuation phase of INH and RIF for four months.

Second-line antitubercular agents are used when patients have drug-resistant TB or cannot tolerate first-line drugs. These include drugs like aminoglycosides (e.g., streptomycin, amikacin), fluoroquinolones (e.g., ofloxacin, moxifloxacin), and injectable bacteriostatic agents (e.g., capreomycin, ethionamide).

It is essential to closely monitor patients undergoing antitubercular therapy for potential side effects and ensure adherence to the treatment regimen to achieve optimal outcomes and prevent the development of drug-resistant strains.

'C3H' is the name of an inbred strain of laboratory mice that was developed at the Jackson Laboratory in Bar Harbor, Maine. The mice are characterized by their uniform genetic background and have been widely used in biomedical research for many decades.

The C3H strain is particularly notable for its susceptibility to certain types of cancer, including mammary tumors and lymphomas. It also has a high incidence of age-related macular degeneration and other eye diseases. The strain is often used in studies of immunology, genetics, and carcinogenesis.

Like all inbred strains, the C3H mice are the result of many generations of brother-sister matings, which leads to a high degree of genetic uniformity within the strain. This makes them useful for studying the effects of specific genes or environmental factors on disease susceptibility and other traits. However, it also means that they may not always be representative of the genetic diversity found in outbred populations, including humans.

A Structure-Activity Relationship (SAR) in the context of medicinal chemistry and pharmacology refers to the relationship between the chemical structure of a drug or molecule and its biological activity or effect on a target protein, cell, or organism. SAR studies aim to identify patterns and correlations between structural features of a compound and its ability to interact with a specific biological target, leading to a desired therapeutic response or undesired side effects.

By analyzing the SAR, researchers can optimize the chemical structure of lead compounds to enhance their potency, selectivity, safety, and pharmacokinetic properties, ultimately guiding the design and development of novel drugs with improved efficacy and reduced toxicity.

Stereoisomerism is a type of isomerism (structural arrangement of atoms) in which molecules have the same molecular formula and sequence of bonded atoms, but differ in the three-dimensional orientation of their atoms in space. This occurs when the molecule contains asymmetric carbon atoms or other rigid structures that prevent free rotation, leading to distinct spatial arrangements of groups of atoms around a central point. Stereoisomers can have different chemical and physical properties, such as optical activity, boiling points, and reactivities, due to differences in their shape and the way they interact with other molecules.

There are two main types of stereoisomerism: enantiomers (mirror-image isomers) and diastereomers (non-mirror-image isomers). Enantiomers are pairs of stereoisomers that are mirror images of each other, but cannot be superimposed on one another. Diastereomers, on the other hand, are non-mirror-image stereoisomers that have different physical and chemical properties.

Stereoisomerism is an important concept in chemistry and biology, as it can affect the biological activity of molecules, such as drugs and natural products. For example, some enantiomers of a drug may be active, while others are inactive or even toxic. Therefore, understanding stereoisomerism is crucial for designing and synthesizing effective and safe drugs.

4-Nitroimidazole at Sigma-Aldrich Edwards, David I. (1993). "Nitroimidazole drugs-action and resistance mechanisms I. Mechanism ... 5-Nitroimidazole is an organic compound with the formula O2NC3H2N2H. The nitro group at position 5 on the imidazole ring is the ... The term nitroimidazole also refers to a class of antibiotics that share similar chemical structures. Imidazole undergoes a ... Nitroimidazole antibiotics have been used to combat anaerobic bacterial and parasitic infections. Perhaps the most common ...
... (EC 3.5.99.9, NnhA, 2NI nitrohydrolase, 2NI denitrase) is an enzyme with systematic name 2- ... nitroimidazole nitrohydrolase. This enzyme catalyses the following chemical reaction 2-nitroimidazole + H2O ⇌ {\displaystyle \ ... 2-nitroimidazole+nitrohydrolase at the U.S. National Library of Medicine Medical Subject Headings (MeSH) Portal: Biology ( ... JS330 Qu Y, Spain JC (April 2011). "Catabolic pathway for 2-nitroimidazole involves a novel nitrohydrolase that also confers ...
Because nitroimidazoles can kill Vibrio cholerae cells, use is not recommended within 14 days of receiving a live cholera ... Like other nitroimidazoles, benznidazole's main mechanism of action is to generate radical species which can damage the ... Benznidazole and other nitroimidazoles have been shown to decrease the rate of clearance of 5-fluorouracil (including 5- ... This limits the spectrum of activity of nitroimidazoles so that host cells and DNA are not also damaged. This mechanism has ...
It was developed in 1972 and is a prominent member of the nitroimidazole antibiotic class. It is on the World Health ... Edwards DI (January 1993). "Nitroimidazole drugs--action and resistance mechanisms. I. Mechanisms of action". The Journal of ... Nitroimidazole antibiotics, Sulfones, World Health Organization essential medicines). ...
It is a nitroimidazole class drug. It used to be commonly added to poultry feed. This led to it being found in eggs. Because of ... Nitroimidazole antibiotics, All stub articles, Antiinfective agent stubs). ...
... is a precursor to the several members of the nitroimidazole antibiotics that are used to combat anaerobic ... Nitroimidazole antibiotics and antiprotozoals containing 2-methylimidazole cores: Dimetridazole Metronidazole Secnidazole ... Edwards, David I (1993). "Nitroimidazole drugs - action and resistance mechanisms. I. Mechanism of action". Journal of ...
The 5-nitroimidazole drugs (metronidazole and tinidazole) are the mainstay of treatment for infection with Trichomonas ... Therapy other than 5-nitroimidazole drugs is also an option, but cure rates are much lower. Oral metronidazole is a treatment ... However, other nitroimidazoles derived from metronidazole such as nimorazole with reduced electron affinity showed less serious ... 2-Methylimidazole is nitrated to give 2-methyl-4(5)-nitroimidazole (2), which is in turn alkylated with ethylene oxide or 2- ...
... is an antibiotic used to treat protozoan infections.: 1368 A synthetic nitroimidazole, it is commercially obtained ... ISBN 978-1-4557-4801-3. Wilcox MH (January 2017), "147 - Nitroimidazoles, Metronidazole, Ornidazole and Tinidazole; and ... Nitroimidazole antibiotics, Organochlorides, Halohydrins, All stub articles, Antiinfective agent stubs, Genito-urinary system ... from an acid-catalyzed reaction between 2-methyl-5-nitroimidazole and epichlorohydrin. Antimicrobial spectrum is similar to ...
... (INN) is a nitroimidazole antifungal medication. It was named in 1984 but apparently never marketed. "Abunidazole ... Nitroimidazoles, Phenols, Tert-butyl compounds, All stub articles, Antiinfective agent stubs). ...
... (INN) is a nitroimidazole anti-infective. It is also being investigated for the treatment of head and neck cancer. ... Nitroimidazole antibiotics, Antiprotozoal agents, 4-Morpholinyl compounds, All stub articles, Antiinfective agent stubs). ...
Other antibiotics that may work include macrolides, lincosamides, nitroimidazoles, and penicillins. Bacterial vaginosis is not ...
... (CL 64855) is a nitroimidazole based drug that cures some protozoan infections. A study of nitroimidazoles found the ... This is despite that other nitroimidazoles proved ineffective against these pathogens.[citation needed] Hall BS, Wilkinson SR ( ... Nitroimidazole antibiotics, Thiadiazoles, All stub articles, Antiinfective agent stubs). ...
It is in the nitroimidazole class of medications. Pretomanid was approved for medical use in the United States in August 2019, ... This class of drug is variously referred to as nitroimidazoles or nitroimidazooxazines. Development of this compound was ...
It is in the nitroimidazole class of medications. Delamanid was approved for medical use in 2014 in Europe, Japan, and South ...
However, if the illness is acute or symptoms persist and medications are needed to treat it, a nitroimidazole medication is ... In the case of nitroimidazole-resistant strains of Giardia, other drugs are available which have showed efficacy in treatment ... Carter ER, Nabarro LE, Hedley L, Chiodini PL (January 2018). "Nitroimidazole-refractory giardiasis: a growing problem requiring ... Resistance has been seen clinically to both nitroimidazoles and albendazole, but not nitazoxanide, though nitazoxanide ...
EF5 is a nitroimidazole derivative used in oncology research. Due to its similarity in chemical structure to etanidazole, EF5 ... Koch CJ (2002). "[1] Measurement of absolute oxygen levels in cells and tissues using oxygen sensors and 2-nitroimidazole EF5 ... February 2003). "Noninvasive imaging of tumor hypoxia in rats using the 2-nitroimidazole 18F-EF5". European Journal of Nuclear ... Lord EM, Harwell L, Koch CJ (December 1993). "Detection of hypoxic cells by monoclonal antibody recognizing 2-nitroimidazole ...
The nitroimidazole antibiotics (usually metronidazole) are the treatments of choice. Treatment usually is successful after 1-2 ... Adriaensen, C.; Claerebout, E.; Martel, A. (June 2014). "Racing Pigeons: A Reservoir for Nitro-Imidazole-Resistant Trichomonas ...
Single oral dose of nitroimidazole is sufficient to kill the parasites. For 95-97% of cases, infection is resolved after one ...
"Predicting nitroimidazole antibiotic resistance mutations in Mycobacterium tuberculosis with protein engineering". PLOS ...
... is in the antiparasitic and the nitroimidazole family of medications. It is believed to work by turning on certain ... a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness". PLOS Neglected ... a New Oral Nitroimidazole Drug Candidate for Treatment of Sleeping Sickness". Antimicrobial Agents and Chemotherapy. American ... Nitroimidazoles, Phenol ethers, Thioethers, World Health Organization essential medicines, Wikipedia medicine articles ready to ...
... (trade names Flagentyl, Sindose, Secnil, Solosec) is a nitroimidazole anti-infective. Effectiveness in the ... Nitroimidazole antibiotics, Antiprotozoal agents, All stub articles, Antiinfective agent stubs). ...
Examples of trypanothione reductase inhibitors include 5-Nitro-Imidazole, Febrifugine, Imipramine and Benzoxaborole. Bond, ...
... is an antiprotozoal drug of the nitroimidazole class used in veterinary medicine. It is used for the treatment of ... Nitroimidazoles, Isopropyl compounds, All stub articles, Antiinfective agent stubs). ...
On entering a viable cell, the nitro group of the FMISO nitroimidazole is reduced. In non-hypoxic cells, the reduced FMISO ... It consists of a 2-nitroimidazole molecule labelled with the positron-emitter fluorine-18. Hypoxia is considered a negative ...
... is a nitroimidazole drug that was investigated in clinical trials for its radiosensitizing properties in cancer ... 18F-EF5, a related nitroimidazole Misonidazole Definition of etanidazole, National Cancer Institute Drug Dictionary. DrugBank ... Nitroimidazoles, All stub articles, Antineoplastic and immunomodulating drug stubs). ...
... is a nitroimidazole derivative used in gynecology for the treatment of trichomonal infections. Marchionni M, ... Nitroimidazole antibiotics, Antiprotozoal agents, Pyrimidines, Alkene derivatives, All stub articles, Antiinfective agent stubs ...
... is a 2-nitroimidazole prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM). Evofosfamide is activated ...
All patients as well as their sexual partners received systemic and/or local nitroimidazole treatment. 61 patients were ...
Nitroimidazole and luminal drugs are paired together when gastrointestinal symptoms caused by amoebiasis are present. ... According to health.harvard.edu, gastrointestinal amoebiasis is treated with nitroimidazole drugs, given orally or ...
Searle had developed Flagyl (metronidazole), a nitroimidazole antibiotic medication used particularly for anaerobic bacteria ...

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