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Trimetrexate
Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor. Uses It has been used with leucovorin in treating pneumocystis pneumonia. It has been investigated for use in treating leiomyosarcoma Leiomyosarcoma is a malignant (cancerous) smooth muscle tumor. A benign tumor originating from the same tissue is termed leiomyoma. While leiomyosarcomas are not thought to arise from leiomyomas, some leiomyoma variants' classification is evolv .... It is a methotrexate (MTX) analog that is active against transport-deficient MTX-resistant tumor cells that overcome the acquired and natural resistance to methotrexate. Other uses include skin lymphoma. Trimetrexate in relapsed T-cell lymphoma with skin involvement. J Clin Oncol. 2002 Jun 15;20(12):2876-80. References External links * * Antifungals Mammalian dihydrofolate reductase inhibitors Protozoal dihydrofolate reductase inhibitors Fungal dihydrofolate reductase inhibitors Quinazolines Antipro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinazoline
Quinazoline is an organic compound with the formula C8H6N2. It is an aromatic heterocycle with a bicyclic structure consisting of two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring. It is a light yellow crystalline solid that is soluble in water. Also known as 1,3-diazanaphthalene, quinazoline received its name from being an aza derivative of quinoline. Though the parent quinazoline molecule is rarely mentioned by itself in technical literature, substituted derivatives have been synthesized for medicinal purposes such as antimalarial and anticancer agents. Quinazoline is a planar molecule. It is isomeric with the other diazanaphthalenes of the benzodiazine subgroup: cinnoline, quinoxaline, and phthalazine. Over 200 biologically active quinazoline and quinoline alkaloids are identified. Synthesis : The synthesis of quinazoline was first reported in 1895 by August Bischler and Lang through the decarboxylation of the 2-carboxy derivative (quinazoline-2-car ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dihydrofolate Reductase Inhibitor
A dihydrofolate reductase inhibitor (DHFR inhibitor) is a molecule that inhibits the function of dihydrofolate reductase, and is a type of antifolate. Since folate is needed by rapidly dividing cells to make thymine, this effect may be used to therapeutic advantage. For example, methotrexate is used as cancer chemotherapy because it can prevent neoplastic cells from dividing. Bacteria also need DHFR to grow and multiply and hence inhibitors selective for bacterial vs. host DHFR have found application as antibacterial agents. An extensive review of the chemical space of small-molecules that inhibit DHFR is summarized in Classes of small-molecules employed as inhibitors of dihydrofolate reductase include diaminoquinazoline and diaminopyrroloquinazoline, Most of the above specified inhibitors are structural analogues of the substrate dihydrofolate and bind to the active site of the enzyme. Further, it has been recently shown that, in ''E. coli'' DHFR, allosteric site binders can in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Leucovorin
Folinic acid, also known as leucovorin, is a medication used to decrease the toxic effects of methotrexate and pyrimethamine. It is also used in combination with 5-fluorouracil to treat colorectal cancer and pancreatic cancer, may be used to treat folate deficiency that results in anemia, and methanol poisoning. It is taken by mouth, injection into a muscle, or injection into a vein. Side effects may include trouble sleeping, allergic reactions, or fever. Use in pregnancy or breastfeeding is generally regarded as safe. When used for anemia it is recommended that pernicious anemia as a cause be ruled out first. Folinic acid is a form of folic acid that does not require activation by dihydrofolate reductase to be useful to the body. Folinic acid was first made in 1945. It is on the World Health Organization's List of Essential Medicines. Medical use Folinic acid is given following methotrexate as part of a total chemotherapeutic plan, where it may protect against bone marr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pneumocystis Pneumonia
''Pneumocystis'' pneumonia (PCP), also known as ''Pneumocystis jirovecii'' pneumonia (PJP), is a form of pneumonia that is caused by the yeast-like fungus ''Pneumocystis jirovecii''. ''Pneumocystis'' specimens are commonly found in the lungs of healthy people although it is usually not a cause for disease. However, they are a source of opportunistic infection and can cause lung infections in people with a weak immune system or other predisposing health conditions. PCP is seen in people with HIV/AIDS (who account for 30-40% of PCP cases), those using medications that suppress the immune system, and people with cancer, autoimmune or inflammatory conditions, and chronic lung disease. Signs and symptoms Signs and symptoms may develop over several days or weeks and may include: shortness of breath and/or difficulty breathing (of gradual onset), fever, dry/non-productive cough, weight loss, night sweats, chills, and fatigue. Uncommonly, the infection may progress to involve other vis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Leiomyosarcoma
Leiomyosarcoma is a malignant (cancerous) smooth muscle tumor. A benign tumor originating from the same tissue is termed leiomyoma. While leiomyosarcomas are not thought to arise from leiomyomas, some leiomyoma variants' classification is evolving. About one in 100,000 people are diagnosed with leiomyosarcoma (LMS) each year. LMS is one of the more common types of soft-tissue sarcoma, representing 10 to 20% of new cases. (Leiomyosarcoma of the bone is more rare.) Sarcoma is rare, consisting of only 1% of cancer cases in adults. Leiomyosarcomas can be very unpredictable; they can remain dormant for long periods of time and recur after years. It is a resistant cancer, meaning generally not very responsive to chemotherapy or radiation. The best outcomes occur when it can be removed surgically with wide margins early, while small and still ''in situ''. Mechanism Smooth muscle cells make up the involuntary muscles, which are found in most parts of the body, including the uterus, s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methotrexate
Methotrexate (MTX), formerly known as amethopterin, is a chemotherapy agent and immune-system suppressant. It is used to treat cancer, autoimmune diseases, and ectopic pregnancies. Types of cancers it is used for include breast cancer, leukemia, lung cancer, lymphoma, gestational trophoblastic disease, and osteosarcoma. Types of autoimmune diseases it is used for include psoriasis, rheumatoid arthritis, and Crohn's disease. It can be given by mouth or by injection. Common side effects include nausea, feeling tired, fever, increased risk of infection, low white blood cell counts, and breakdown of the skin inside the mouth. Other side effects may include liver disease, lung disease, lymphoma, and severe skin rashes. People on long-term treatment should be regularly checked for side effects. It is not safe during breastfeeding. In those with kidney problems, lower doses may be needed. It acts by blocking the body's use of folic acid. Methotrexate was first made in 1947 and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antifungals
An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually yes obtained by a doctor's prescription, but a few are available over the counter (OTC). Types of antifungal There are two types of antifungals: local and systemic. Local antifungals are usually administered topically or vaginally, depending on the condition being treated. Systemic antifungals are administered orally or intravenously. Of the clinically employed azole antifungals, only a handful are used systemically. These include ketoconazole, itraconazole, fluconazole, fosfluconazole, voriconazole, posaconazole, and isavuconazole. Examples of non-azole systemic antifungals include griseofulvin and terbinafine. Classes Polyenes A polyene is a molecule with multiple conjugated do ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mammalian Dihydrofolate Reductase Inhibitors
Mammals () are a group of vertebrate animals constituting the class Mammalia (), characterized by the presence of mammary glands which in females produce milk for feeding (nursing) their young, a neocortex (a region of the brain), fur or hair, and three middle ear bones. These characteristics distinguish them from reptiles (including birds) from which they diverged in the Carboniferous, over 300 million years ago. Around 6,400 extant species of mammals have been described divided into 29 orders. The largest orders, in terms of number of species, are the rodents, bats, and Eulipotyphla (hedgehogs, moles, shrews, and others). The next three are the Primates (including humans, apes, monkeys, and others), the Artiodactyla ( cetaceans and even-toed ungulates), and the Carnivora (cats, dogs, seals, and others). In terms of cladistics, which reflects evolutionary history, mammals are the only living members of the Synapsida (synapsids); this clade, together with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protozoal Dihydrofolate Reductase Inhibitors
Protozoa (singular: protozoan or protozoon; alternative plural: protozoans) are a group of single-celled eukaryotes, either free-living or parasitic, that feed on organic matter such as other microorganisms or organic tissues and debris. Historically, protozoans were regarded as "one-celled animals", because they often possess animal-like behaviours, such as motility and predation, and lack a cell wall, as found in plants and many algae. When first introduced by Georg Goldfuss (originally spelled Goldfuß) in 1818, the taxon Protozoa was erected as a class within the Animalia, with the word 'protozoa' meaning "first animals". In later classification schemes it was elevated to a variety of higher ranks, including phylum, subkingdom and kingdom, and sometimes included within Protoctista or Protista. The approach of classifying Protozoa within the context of Animalia was widespread in the 19th and early 20th century, but not universal. By the 1970s, it became usual to require ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fungal Dihydrofolate Reductase Inhibitors
A fungus ( : fungi or funguses) is any member of the group of eukaryotic organisms that includes microorganisms such as yeasts and molds, as well as the more familiar mushrooms. These organisms are classified as a kingdom, separately from the other eukaryotic kingdoms, which by one traditional classification include Plantae, Animalia, Protozoa, and Chromista. A characteristic that places fungi in a different kingdom from plants, bacteria, and some protists is chitin in their cell walls. Fungi, like animals, are heterotrophs; they acquire their food by absorbing dissolved molecules, typically by secreting digestive enzymes into their environment. Fungi do not photosynthesize. Growth is their means of mobility, except for spores (a few of which are flagellated), which may travel through the air or water. Fungi are the principal decomposers in ecological systems. These and other differences place fungi in a single group of related organisms, named the ''Eumycota'' (''true f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinazolines
Quinazoline is an organic compound with the formula C8H6N2. It is an aromatic heterocycle with a bicyclic structure consisting of two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring. It is a light yellow crystalline solid that is soluble in water. Also known as 1,3-diazanaphthalene, quinazoline received its name from being an aza derivative of quinoline. Though the parent quinazoline molecule is rarely mentioned by itself in technical literature, substituted derivatives have been synthesized for medicinal purposes such as antimalarial and anticancer agents. Quinazoline is a planar molecule. It is isomeric with the other diazanaphthalenes of the benzodiazine subgroup: cinnoline, quinoxaline, and phthalazine. Over 200 biologically active quinazoline and quinoline alkaloids are identified. Synthesis : The synthesis of quinazoline was first reported in 1895 by August Bischler and Lang through the decarboxylation of the 2-carboxy derivative (quinazoline- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiprotozoal Agents
Antiprotozoal agents ( ATC code: ATC P01) is a class of pharmaceuticals used in treatment of protozoan infection. A paraphyletic group, protozoans have little in common with each other. For example, ''Entamoeba histolytica'', a unikont eukaryotic organism, is more closely related to ''Homo sapiens'' (humans), which also belongs to the unikont phylogenetic group, than it is to ''Naegleria fowleri'', a "protozoan" bikont. As a result, agents effective against one pathogen may not be effective against another. Antiprotozoal agents can be grouped by mechanism or by organism. Recent papers have also proposed the use of viruses to treat infections caused by protozoa. Medical uses Antiprotozoals are used to treat protozoal infections, which include amebiasis, giardiasis, cryptosporidiosis, microsporidiosis, malaria, babesiosis, trypanosomiasis, Chagas disease, leishmaniasis, and toxoplasmosis. Currently, many of the treatments for these infections are limited by their toxicity. Outdat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
