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Oxazolidinones
2-Oxazolidinone is a heterocyclic organic compound containing both nitrogen and oxygen in a 5-membered ring. Synthesis and occurrence The compound arises by the reaction of an ethanolamine and dimethylcarbonate or related phosgene equivalents. It is one of waste products generated in amine gas treating due to cyclization of ethanolamine carbamate. History The compound was first reported in 1888 by German chemist Siegmund Gabriel. While investigating reactions of bromoethylamine hydrobromide, he treated it with silver carbonate and isolated a product with melting point around 90–91°C. He determined its empirical formula correctly, but neither gave it a specific name not studied its properties. Nine years later Gabriel returned to the topic together with G. Eschenbach, developing a more efficient synthesis using sodium bicarbonate instead of the silver salt. They referred to the compound as "Oxäthylcarbaminsäureanhydrid" (hydroxyethylcarbamic acid anhydride), recognizing it ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Linezolid
Linezolid is an antibiotic used for the treatment of infections caused by Gram-positive bacteria that are resistant to other antibiotics. Linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant ''Staphylococcus aureus'' (MRSA). The main uses are infections of the skin and pneumonia although it may be used for a variety of other infections including drug-resistant tuberculosis. It is used either by injection into a vein or by mouth. When given for short periods, linezolid is a relatively safe antibiotic. It can be used in people of all ages and in people with liver disease or poor kidney function. Common side effects with short-term use include headache, diarrhea, rash, and nausea. Serious side effects may include serotonin syndrome, bone marrow suppression, and high blood lactate levels, particularly when used for more than two weeks. If used for longer period ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxazolidinones
2-Oxazolidinone is a heterocyclic organic compound containing both nitrogen and oxygen in a 5-membered ring. Synthesis and occurrence The compound arises by the reaction of an ethanolamine and dimethylcarbonate or related phosgene equivalents. It is one of waste products generated in amine gas treating due to cyclization of ethanolamine carbamate. History The compound was first reported in 1888 by German chemist Siegmund Gabriel. While investigating reactions of bromoethylamine hydrobromide, he treated it with silver carbonate and isolated a product with melting point around 90–91°C. He determined its empirical formula correctly, but neither gave it a specific name not studied its properties. Nine years later Gabriel returned to the topic together with G. Eschenbach, developing a more efficient synthesis using sodium bicarbonate instead of the silver salt. They referred to the compound as "Oxäthylcarbaminsäureanhydrid" (hydroxyethylcarbamic acid anhydride), recognizing it ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rivaroxaban
Rivaroxaban, sold under the brand name Xarelto among others, is an anticoagulant medication (blood thinner) used to treat and reduce the risk of blood clots. Specifically it is used to treat deep vein thrombosis and pulmonary emboli and prevent blood clots in atrial fibrillation and following hip or knee surgery. It is taken by mouth. Common side effects include bleeding. Other serious side effects may include spinal hematoma and anaphylaxis. It is unclear if use in pregnancy and breastfeeding is safe. Compared to warfarin it has fewer interactions with other medications. It works by blocking the activity of the clotting protein factor Xa. Rivaroxaban was patented in 2007 and approved for medical use in the United States in 2011. It is available as a generic medication. It is on the World Health Organization's List of Essential Medicines. In 2022, it was the 90th most commonly prescribed medication in the United States, with more than 7million prescriptions. Medical use ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein Synthesis Inhibitor
A protein synthesis inhibitor is a compound that stops or slows the growth or proliferation of cells by disrupting the processes that lead directly to the generation of new proteins. While a broad interpretation of this definition could be used to describe nearly any compound depending on concentration, in practice, it usually refers to compounds that act at the molecular level on translational machinery (either the ribosome itself or the translation factor), taking advantages of the major differences between prokaryotic and eukaryotic ribosome structures. Mechanism In general, protein synthesis inhibitors work at different stages of bacterial translation, bacterial mRNA translation into proteins, like initiation, elongation (including aminoacyl tRNA entry, Proofreading (biology), proofreading, peptidyl transfer, and bacterial translation#Elongation, bacterial translocation) and termination: Earlier stages * Rifamycin inhibits Bacterial transcription, bacterial DNA transcription ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aldol Reaction
The aldol reaction (aldol addition) is a Chemical reaction, reaction in organic chemistry that combines two Carbonyl group, carbonyl compounds (e.g. aldehydes or ketones) to form a new β-hydroxy carbonyl compound. Its simplest form might involve the nucleophilic addition of an Enolate, enolized ketone to another: These products are known as ''aldols'', from the ''ald''ehyde + alcoh''ol'', a structural motif seen in many of the products. The use of aldehyde in the name comes from its history: aldehydes are more reactive than ketones, so that the reaction was discovered first with them. The aldol reaction is paradigmatic in organic chemistry and one of the most common means of forming carbon–carbon bonds in organic chemistry. It lends its name to the family of aldol reactions and similar techniques analyze a whole family of carbonyl α-substitution reactions, as well as the Claisen condensation, diketone condensations. Scope Aldol structural units are found in many importa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxazolone
Oxazolone is a chemical compound and functional group, with the molecular formula C3H3NO2. It was named in-line with the Hantzsch–Widman nomenclature and is part of a large family of oxazole based compounds. There are a total of 5 structural isomers of oxazolone; 3 according to the location of the carbonyl group and 2 more according to the location of the double bond C=X (with X= N or C): *2-(3''H'')oxazolone *2-(5''H'')oxazolone *4-(5''H'')-oxazolone *5-(2''H'')-oxazolone *5-(4''H'')-oxazolone The 4-oxazolone motif, which is also formally a lactam, is present in a number of drugs (fenozolone, thozalinone, cyclazodone, reclazepam etc.). Substituted 5-oxazolones may also be regarded as the cyclization products of ''N''-acyl α-amino acids, making them lactones, and are sometimes referred to as azlactones. See also * Münchnone * Oxazole * Oxazolidone — the saturated analogues References {{reflist Oxazolones ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Contezolid
Contezolid (trade name Youxitai) is an antibiotic of the oxazolidinone class. It is effective against ''Staphylococcus aureus'', methicillin-resistant ''Staphylococcus aureus'' (MRSA), ''Streptococcus pyogenes'', ''Streptococcus agalactiae'', and other bacteria. In 2021, it was approved by the National Medical Products Administration of China for the treatment of complicated skin and soft tissue infections (cSSTI). A prodrug of contezolid, contezolid acefosamil, which is formulated for IV administration Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutr ... is in Phase III clinical trials for diabetic foot infection. : References {{reflist Oxazolidinone antibiotics Oxazoles Fluoroarenes Secondary amines Tetrahydropyridines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Radezolid
Radezolid (INN, codenamed RX-1741) is a novel oxazolidinone The oxazolidones and isoxazolidones are a set of six isomeric five-membered heterocyclic compounds consisting of a carbonyl group, an oxygen atom, a nitrogen atom with a hydrogen atom attached, and two methylene groups. The chemicals differ in the ... antibiotic being developed by Melinta Therapeutics, Inc. for the treatment of bacterial acne. References Further reading * * * * * * Oxazolidinone antibiotics Triazoles Fluoroarenes Acetamides Biphenyls {{antibiotic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tedizolid
Tedizolid, sold under the brand name Sivextro (by Merck) is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics (originator: Dong-A Pharmaceuticals), and is marketed for the treatment of acute bacterial skin and skin structure infections (also known as complicated skin and skin-structure infections (cSSSIs)). The most common side effects include nausea (feeling sick), headache, Diarrhea, diarrhoea and vomiting. These side effects were generally of mild or moderate severity. Tedizolid was approved for medical use by the FDA in the United States in June 2014, and for medical use in the European Union by European Medicines Agency, EMA in March 2015. Medical uses Tedizolid was approved by the U.S Food and Drug Administration (FDA) on June 20, 2014, with the indication for the treatment of acute bacterial Skin and skin structure i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Posizolid
Posizolid is an oxazolidinone antibiotic under investigation by AstraZeneca for the treatment of bacterial infections. At a concentration of 2 mg/L it inhibited 98% of all Gram-positive bacteria tested in vitro ''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in .... References Oxazolidinone antibiotics Isoxazoles Ethers Fluoroarenes Tetrahydropyridines Carboxamides Vicinal diols {{antibiotic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via routes other than intravenous, its bioavailability is lower due to intestinal epithelium absorption and first-pass metabolism. Thereby, mathematically, bioavailability equals the ratio of comparing the area under the plasma drug concentration curve versus time (AUC) for the extravascular formulation to the AUC for the intravascular formulation. AUC is used because AUC is proportional to the dose that has entered the systemic circulation. Bioavailability of a drug is an average value; to take population variability into account, deviation range is shown as ±. To ensure that the drug taker who has poor absorption is dosed appropriately, the bottom value of the deviation range is employed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
