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Diverted Total Synthesis
Diverted total synthesis in chemistry is a strategy in drug discovery aiming at organic synthesis of natural product analogues rather than the natural product itself. The target can be the modification of a natural product or the modification of an intermediate. In this sense it differs from other strategies such as total synthesis and semisynthesis. The purpose can be gaining a scientific understanding of the biological activity of the original natural product or the discovery of new drugs with the same biological activity but simpler to produce. The concept was introduced by Samuel J. Danishefsky in 2006. Notable examples of this strategy are the potential drug ixabepilone which is an analogue of the natural product epothilone B and carfilzomib which is derived from epoxomicin and eravacycline derived from tetracycline. Cabergoline is derived from a number of ergot alkaloids one of which is lysergic acid and Simvastatin is based on Lovastatin. Diverted total synthesis is a t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemistry
Chemistry is the scientific study of the properties and behavior of matter. It is a physical science within the natural sciences that studies the chemical elements that make up matter and chemical compound, compounds made of atoms, molecules and ions: their composition, structure, properties, behavior and the changes they undergo during chemical reaction, reactions with other chemical substance, substances. Chemistry also addresses the nature of chemical bonds in chemical compounds. In the scope of its subject, chemistry occupies an intermediate position between physics and biology. It is sometimes called the central science because it provides a foundation for understanding both Basic research, basic and Applied science, applied scientific disciplines at a fundamental level. For example, chemistry explains aspects of plant growth (botany), the formation of igneous rocks (geology), how atmospheric ozone is formed and how environmental pollutants are degraded (ecology), the prop ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lysergic Acid
Lysergic acid, also known as -lysergic acid and (+)-lysergic acid, is a precursor for a wide range of ergoline alkaloids that are produced by the ergot fungus and found in the seeds of '' Argyreia nervosa'' ( Hawaiian baby woodrose), and ''Ipomoea'' species ( morning glories, ololiuhqui, tlitliltzin). Amides of lysergic acid, lysergamides, are widely used as pharmaceuticals and as psychedelic drugs, e.g. lysergic acid diethylamide (LSD). Lysergic acid is listed as a Table I precursor under the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. The name Lysergic acid comes from the fact that it is a carboxylic acid, and it was first made by hydrolysis of various ergot alkaloids. Synthesis Laboratory Lysergic acid is generally produced by hydrolysis of natural lysergamides, but can also be synthesized in the laboratory by a complex total synthesis, for example by Robert Burns Woodward's team in 1956. An enantioselective total ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lysergic Acid Chemical Structure
Lysergic acid, also known as -lysergic acid and (+)-lysergic acid, is a precursor for a wide range of ergoline alkaloids that are produced by the ergot fungus and found in the seeds of ''Argyreia nervosa'' ( Hawaiian baby woodrose), and ''Ipomoea'' species (morning glories, ololiuhqui, tlitliltzin). Amides of lysergic acid, lysergamides, are widely used as pharmaceuticals and as psychedelic drugs, e.g. lysergic acid diethylamide (LSD). Lysergic acid is listed as a Table I precursor under the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. The name Lysergic acid comes from the fact that it is a carboxylic acid, and it was first made by hydrolysis of various ergot alkaloids. Synthesis Laboratory Lysergic acid is generally produced by hydrolysis of natural lysergamides, but can also be synthesized in the laboratory by a complex total synthesis, for example by Robert Burns Woodward's team in 1956. An enantioselective total sy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetracycline
Tetracycline, sold under various brand names, is an antibiotic in the tetracyclines family of medications, used to treat a number of infections, including acne, cholera, brucellosis, plague, malaria, and syphilis. It is available in oral and topical formulations. Common side effects include vomiting, diarrhea, rash, and loss of appetite. Other side effects include poor tooth development if used by children less than eight years of age, kidney problems, and sunburning easily. Use during pregnancy may harm the baby. It works by inhibiting protein synthesis in bacteria. Tetracycline was patented in 1953 and was approved for prescription use in 1954. It is on the World Health Organization's List of Essential Medicines. Tetracycline is available as a generic medication. Tetracycline was originally made from bacteria of the genus ''Streptomyces''. Medical uses Spectrum of activity Tetracyclines have a broad spectrum of antibiotic action. Originally, they possessed some lev ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eravacycline
Eravacycline (TP-434, Xerava) is a synthetic halogenated tetracycline class antibiotic by Tetraphase Pharmaceuticals. It is closely related to tigecycline. It has a broad spectrum of activity including many multi-drug resistant strains of bacteria. Phase III studies in complicated intra-abdominal infections (cIAI) and complicated urinary tract infections (cUTI) were recently completed with mixed results. Eravacycline was granted fast track designation by the FDA and is currently available in USA. Medical uses Eravacycline has shown broad spectrum of activity against a variety of Gram-positive and Gram-negative bacteria, including multi-drug resistant strains, such as methicillin-resistant ''Staphylococcus aureus'' (MRSA) and carbapenem-resistant Enterobacteriaceae. It is currently being formulated as for intravenous and oral administration. Spectrum of activity Gram-positive organisms * ''Staphylococcus aureus'' (both methicillin-resistant and sensitive strains) * ''S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetracycline Skeletal
Tetracycline, sold under various brand names, is an antibiotic in the tetracyclines family of medications, used to treat a number of infections, including acne, cholera, brucellosis, plague, malaria, and syphilis. It is available in oral and topical formulations. Common side effects include vomiting, diarrhea, rash, and loss of appetite. Other side effects include poor tooth development if used by children less than eight years of age, kidney problems, and sunburning easily. Use during pregnancy may harm the baby. It works by inhibiting protein synthesis in bacteria. Tetracycline was patented in 1953 and was approved for prescription use in 1954. It is on the World Health Organization's List of Essential Medicines. Tetracycline is available as a generic medication. Tetracycline was originally made from bacteria of the genus ''Streptomyces''. Medical uses Spectrum of activity Tetracyclines have a broad spectrum of antibiotic action. Originally, they possessed some leve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eravacycline Structure
Eravacycline (TP-434, Xerava) is a synthetic halogenated tetracycline class antibiotic by Tetraphase Pharmaceuticals. It is closely related to tigecycline. It has a broad spectrum of activity including many multi-drug resistant strains of bacteria. Phase III studies in complicated intra-abdominal infections (cIAI) and complicated urinary tract infections (cUTI) were recently completed with mixed results. Eravacycline was granted fast track designation by the FDA and is currently available in USA. Medical uses Eravacycline has shown broad spectrum of activity against a variety of Gram-positive and Gram-negative bacteria, including multi-drug resistant strains, such as methicillin-resistant ''Staphylococcus aureus'' (MRSA) and carbapenem-resistant Enterobacteriaceae. It is currently being formulated as for intravenous and oral administration. Spectrum of activity Gram-positive organisms * ''Staphylococcus aureus'' (both methicillin-resistant and sensitive strains) * ''S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carfilzomib
Carfilzomib, sold under the brand name Kyprolis, is an anti-cancer medication acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin. It was developed by Onyx Pharmaceuticals. The US Food and Drug Administration (FDA) approved it in July 2012. Medical uses The FDA approved carfilzomib in July 2012, for use in people with multiple myeloma who have received at least two prior therapies, including treatment with bortezomib and an immunomodulatory therapy (such as lenalidomide) and have demonstrated disease progression on or within 60 days of completion of the last therapy. Mechanism Carfilzomib covalently irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme that degrades unwanted cellular proteins. Carfilzomib displays minimal interactions with non-proteasomal targets, thereby improving safety profiles over bortezomib. Inhibition of proteasome-mediated proteolysis resu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epoxomicin
Epoxomicin is a naturally occurring selective proteasome inhibitor with anti-inflammatory activity. It was originally discovered in 1992. Peptide Institute, Inc. Injected, it can induce -like symptoms in rats. Derivatives of epoxomicin include carfilzomib
Carfilzomib, sold under the brand name Kyprolis, is an anti-cancer medication acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin. It was developed by Onyx Pharmaceuticals.
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Carfilzomib Structure
Carfilzomib, sold under the brand name Kyprolis, is an anti-cancer medication acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin. It was developed by Onyx Pharmaceuticals. The US Food and Drug Administration (FDA) approved it in July 2012. Medical uses The FDA approved carfilzomib in July 2012, for use in people with multiple myeloma who have received at least two prior therapies, including treatment with bortezomib and an immunomodulatory therapy (such as lenalidomide) and have demonstrated disease progression on or within 60 days of completion of the last therapy. Mechanism Carfilzomib covalently irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme that degrades unwanted cellular proteins. Carfilzomib displays minimal interactions with non-proteasomal targets, thereby improving safety profiles over bortezomib. Inhibition of proteasome-mediated proteolysis results ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epothilone B
Epothilones are a class of potential cancer drugs. Like taxanes, they prevent cancer cells from dividing by interfering with tubulin, but in early trials, epothilones have better efficacy and milder adverse effects than taxanes. Epothilones were originally identified as metabolites produced by the soil-dwelling myxobacterium ''Sorangium cellulosum''. , epothilones A to F have been identified and characterized. Early studies in cancer cell lines and human cancer patients indicate superior efficacy to the taxanes. Their mechanism of action is similar, but their chemical structure is simpler. Due to their better water solubility, cremophors (solubilizing agents used for paclitaxel which can affect cardiac function and cause severe hypersensitivity) are not needed. Endotoxin-like properties known from paclitaxel, like activation of macrophages synthesizing inflammatory cytokines and nitric oxide, are not observed for epothilone B. History The structure of epothilone A was determin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
