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Diaminopyrimidine
Diaminopyrimidines (DAP) are a class of organic chemical compounds that include two amine groups on a pyrimidine ring. They include many dihydrofolate reductase inhibitor drugs (such as pyrimethamine, trimetrexate, and piritrexim and the antibiotics iclaprim and trimethoprim). Some have been patented as anti-cancer drugs. See also * 2,4-Diaminopyrimidine * 4,5-Diaminopyrimidine References Aminopyrimidines {{organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2,4-Diaminopyrimidine
2,4-Diaminopyrimidine is an organic compound with the formula . It is the parent of one isomer of the diaminopyrimidines. Such compounds are structurally related to folic acid and the basis of much medicinal chemistry including the drug pyrimethamine. Further reading * See also * 4,5-Diaminopyrimidine References {{DEFAULTSORT:Diaminopyrimidine, 2,4- Nucleobases Aminopyrimidines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4,5-Diaminopyrimidine
4,5-Diaminopyrimidine is a diaminopyrimidine. See also * 2,4-Diaminopyrimidine 2,4-Diaminopyrimidine is an organic compound with the formula . It is the parent of one isomer of the diaminopyrimidines. Such compounds are structurally related to folic acid and the basis of much medicinal chemistry including the drug pyrimetha ... References Aminopyrimidines {{aromatic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trimethoprim
Trimethoprim (TMP) is an antibiotic used mainly in the treatment of bladder infections. Other uses include for middle ear infections and travelers' diarrhea. With sulfamethoxazole or dapsone it may be used for ''Pneumocystis'' pneumonia in people with HIV/AIDS. It is taken orally (swallowed by mouth). Common side effects include nausea, changes in taste, and rash. Rarely it may result in blood problems such as not enough platelets or white blood cells. Trimethoprim may cause sun sensitivity. There is evidence of potential harm during pregnancy in some animals but not humans. It works by blocking folate metabolism via dihydrofolate reductase in some bacteria, preventing creation of bacterial DNA and RNA and leading to bacterial cell death. Trimethoprim was first used in 1962. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication. Medical uses It is primarily used in the treatment of urinary tract infectio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Organic Chemical
Some chemical authorities define an organic compound as a chemical compound that contains a Carbon–hydrogen bond, carbon–hydrogen or carbon–carbon bond; others consider an organic compound to be any chemical compound that contains carbon. For example, carbon-containing compounds such as alkanes (e.g. methane ) and its derivatives are universally considered organic, but many others are sometimes considered Inorganic compound, inorganic, such as certain compounds of carbon with nitrogen and oxygen (e.g. cyanide ion , hydrogen cyanide , chloroformic acid , carbon dioxide , and carbonate ion ). Due to carbon's ability to catenate (form chains with other carbon atoms), millions of organic compounds are known. The study of the properties, reactions, and syntheses of organic compounds comprise the discipline known as organic chemistry. For historical reasons, a few classes of carbon-containing compounds (e.g., carbonate salts and cyanide salts), along with a few other exceptions (e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amine
In chemistry, amines (, ) are organic compounds that contain carbon-nitrogen bonds. Amines are formed when one or more hydrogen atoms in ammonia are replaced by alkyl or aryl groups. The nitrogen atom in an amine possesses a lone pair of electrons. Amines can also exist as hetero cyclic compounds. Aniline is the simplest aromatic amine, consisting of a benzene ring bonded to an amino group. Amines are classified into three types: primary (1°), secondary (2°), and tertiary (3°) amines. Primary amines (1°) contain one alkyl or aryl substituent and have the general formula RNH2. Secondary amines (2°) have two alkyl or aryl groups attached to the nitrogen atom, with the general formula R2NH. Tertiary amines (3°) contain three substituent groups bonded to the nitrogen atom, and are represented by the formula R3N. The functional group present in primary amines is called the amino group. Classification of amines Amines can be classified according to the nature and number o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrimidine
Pyrimidine (; ) is an aromatic, heterocyclic, organic compound similar to pyridine (). One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has nitrogen atoms at positions 1 and 3 in the ring. The other diazines are pyrazine (nitrogen atoms at the 1 and 4 positions) and pyridazine (nitrogen atoms at the 1 and 2 positions). In nucleic acids, three types of nucleobases are pyrimidine derivatives: cytosine (C), thymine (T), and uracil (U). Occurrence and history The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. It is also found in many synthetic compounds such as barbiturates and the HIV drug zidovudine. Although pyrimidine derivatives such as alloxan were known in the early 19th century, a laboratory synthesis of a pyrimidine was not carried out until 1879, when Grimaux repor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Iclaprim
Iclaprim is an antibiotic drug candidate that is active against Gram positive organisms. It is administered intravenously. ''In vitro'', iclaprim is active against methicillin-resistant ''Staphylococcus aureus'' (MRSA), vancomycin-resistant ''Staphylococcus aureus'' (VRSA), strains of ''Streptococcus pneumoniae'' resistant to several common antibiotics, and some Gram-negative bacteria. It is of the diaminopyrimidine dihydrofolate reductase (DHFR)- inhibiting type. History Iclaprim is an optimized analog of trimethoprim that was discovered by scientists at Roche. Arpida was spun out of Roche in 1998, and acquired iclaprim from Roche in 2001. Arpida held an initial public offering on the Swiss stock exchange in 2005. Arpida ran two Phase III clinical trials for complicated skin and skin structure infections that were completed by 2008, but as of 2017, had not been published in the medical literature. A new drug application was filed with the United States Food and Drug Admi ... [...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. 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 inhibit the enzyme either uncompetitively or non-competitively. The examples provided below are sp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrimethamine
Pyrimethamine, sold under the brand name Daraprim among others, is a medication used with leucovorin (leucovorin is used to decrease side effects of pyrimethamine; it does not have intrinsic anti-parasitic activity) to treat the parasitic diseases toxoplasmosis and cystoisosporiasis. It is also used with dapsone as a second-line option to prevent Pneumocystis pneumonia, ''Pneumocystis jiroveci'' pneumonia in people with HIV/AIDS. It was previously used for malaria but is no longer recommended due to resistance. Pyrimethamine is oral administration, taken by mouth. Common side effects include gastrointestinal upset, severe allergic reactions, and bone marrow suppression. It should not be used by people with folate deficiency that has resulted in anemia. There is concern that it may increase the risk of cancer. While occasionally used in pregnancy it is unclear if pyrimethamine is safe for the baby. Pyrimethamine is classified as a folic acid antagonist. It works by inhibiting f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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. It is a methotrexate Methotrexate, formerly known as amethopterin, is a chemotherapy agent and immunosuppressive drug, immune-system suppressant. It is used to treat cancer, autoimmune diseases, and ectopic pregnancy, ectopic pregnancies. Types of cancers it is u ... (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 Antiprot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
