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Spiroindolone
The spiroindolones are a class of compounds in which an indolone ring is substituted with another ring in a spiro arrangement. Alkaloids in this class include horsfiline, rhynchophylline, gelsemine, carapanaubine, and maremycin E. Spiroindolones are also an emerging class of antimalarial drugs whose mode of action is to inhibit protein synthesis in the target parasite. The most advanced compound in this class in terms of drug development Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regu ... is cipargamin (NITD609). References Antimalarial agents Spiro compounds {{antiinfective-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cipargamin
Cipargamin (NITD609, KAE609) is an experimental synthetic antimalarial drug belonging to the spiroindolone class. The compound was developed at the Novartis Institute for Tropical Diseases in Singapore, through a collaboration with the Genomics Institute of the Novartis Research Foundation (GNF), the Biomedical Primate Research Centre and the Swiss Tropical Institute. Cipargamin is a synthetic antimalarial molecule belonging to the spiroindolone class, awarded MMV Project of the Year 2009. It is structurally related to GNF 493, a compound first identified as a potent inhibitor of ''Plasmodium falciparum'' growth in a high throughput phenotypic screen of natural products conducted at the Genomics Institute of the Novartis Research Foundation in San Diego, California in 2006. Cipargamin was discovered by screening the Novartis library of 12,000 natural products and synthetic compounds to find compounds active against ''Plasmodium falciparum''. The first screen turned up 275 compound ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Horsfiline
Horsfiline is an oxindole alkaloid found in the plant '' Horsfieldia superba'', which is used in traditional herbal medicine. It has analgesic effects and has been the subject of research both to produce it synthetically by convenient routes and to develop analogues and derivatives which may have improved analgesic effects. It is a member of the spiroindolone The spiroindolones are a class of compounds in which an indolone ring is substituted with another ring in a spiro arrangement. Alkaloids in this class include horsfiline, rhynchophylline, gelsemine, carapanaubine, and maremycin E. Spiroind ... class. Elacomine has a similar chemical structure. References {{reflist Phenol ethers Lactams Oxindoles Pyrrolidine alkaloids Spiro compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indolone
Oxindole (2-indolone) is an aromatic heterocyclic organic compound with the formula . It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered nitrogen-containing ring. Oxindole is a modified indoline with a substituted carbonyl at the second position of the 5-member indoline ring. Classified as a cyclic amide, it is a pale yellow solid. Formation and reactions Oxindole is derived in nature from tryptophan, formed by gut bacteria ("normal flora"). It is normally metabolized and detoxified from the body by the liver. In excess, it can cause sedation, muscle weakness, hypotension, and coma. Patients with hepatic encephalopathy have been recorded to have elevated serum oxindole levels. Treatment with phosphorus pentasulfide gives the thione. Oxindoles Beyond the parent compound, the oxindole structure is present in many compounds including, for example, rhynchophylline, 3-methyloxindole, and semaxanib Semaxanib (INN, codenamed SU5416) is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spiro Compound
In organic chemistry, spiro compounds are Organic compound, compounds that have at least two Cyclic compound, molecular rings sharing one common atom. Simple spiro compounds are bicyclic (having just two rings). The presence of only one common atom connecting the two rings distinguishes spiro compounds from other bicyclics.For all four categories, see The specific chapters can be found aan respectively, same access date. For the description featuring adjacent atoms for all but the isolated category, see Clayden, op. cit. Spiro compounds may be fully carbocyclic (all carbon) or heterocyclic (having one or more non-carbon atom). One common type of spiro compound encountered in educational settings is a heterocyclic one— the acetal formed by reaction of a diol with a cyclic ketone. The common atom that connects the two (or sometimes three) rings is called the ''spiro atom''. In carbocyclic spiro compounds like spiro[5.5]undecane, the spiro-atom is a quaternary carbon, and as the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkaloid
Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large variety of organisms including bacteria, fungus, fungi, Medicinal plant, plants, and animals. They can be purified from crude extracts of these organisms by acid-base extraction, or solvent extractions followed by silica-gel column chromatography. Alkaloids have a wide range of pharmacology, pharmacological activities including antimalarial medication, antimalarial (e.g. quinine), asthma, antiasthma (e.g. ephedrine), chemotherapy, anticancer (e.g. omacetaxine mepesuccinate, homoharringtonine), cholinomimetic (e.g. galantamine), vasodilation, vasodilatory (e.g. vincamine), Antiarrhythmic agent, antiarrhythmic (e.g. quinidine), analgesic (e.g. morphine), antibacterial (e.g. chelerythrine), and anti-diabetic, antihyperglycemic activities (e.g. berb ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rhynchophylline
Rhynchophylline is an alkaloid found in certain ''Uncaria'' species (Rubiaceae), notably '' Uncaria rhynchophylla'' and '' Uncaria tomentosa''. It also occurs in the leaves of '' Mitragyna speciosa'' (kratom) and Mitragyna tubulosa, a tree native to Thailand. Chemically, it is related to the alkaloid mitragynine. Rhynchophylline is a non-competitive NMDA antagonist (IC50 = 43.2 μM) and a calcium channel blocker. ''Uncaria'' species have had a variety of uses in traditional herbal medicine, such as for lightheadedness, convulsions, numbness, and hypertension. These uses have been associated with the presence of rhynchophylline and have encouraged its investigation as a drug candidate for several cardiovascular and central nervous system diseases; however, few clinically relevant studies have been conducted. See also *Ibotenic acid Ibotenic acid or (''S'')-2-amino-2-(3-hydroxyisoxazol-5-yl)acetic acid, also referred to as ibotenate, is a naturally occurring alpha-amino a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gelsemine
Gelsemine (C20H22N2O2) is an indole alkaloid isolated from flowering plants of the genus ''Gelsemium sempervirens, Gelsemium'', a plant native to the subtropical and tropical Americas, and southeast Asia, and is a highly toxic compound that acts as a paralytic, exposure to which can result in death. It has generally potent activity as an agonist of the mammalian glycine receptor, the activation of which leads to an inhibitory postsynaptic potential in neurons following chloride ion influx, and systemically, to muscle relaxation of varying intensity and deleterious effect. Despite its danger and toxicity, recent pharmacological research has suggested that the biological activities of this compound may offer opportunities for developing treatments related to xenobiotic or diet-induced oxidative stress, and of anxiety and other conditions, with ongoing research including attempts to identify safer derivatives and analogs to make use of gelsemine's beneficial effects. Natural source ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antimalarial Drug
Antimalarial medications or simply antimalarials are a type of antiparasitic chemical agent, often naturally derived, that can be used to treat or to prevent malaria, in the latter case, most often aiming at two susceptible target groups, young children and pregnant women. As of 2018, modern treatments, including for severe malaria, continued to depend on therapies deriving historically from quinine and artesunate, both parenteral (injectable) drugs, expanding from there into the many classes of available modern drugs. Incidence and distribution of the disease ("malaria burden") is expected to remain high, globally, for many years to come; moreover, known antimalarial drugs have repeatedly been observed to elicit resistance in the malaria parasite—including for combination therapies featuring artemisinin, a drug of last resort, where resistance has now been observed in Southeast Asia. As such, the needs for new antimalarial agents and new strategies of treatment (e.g., new com ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Development
Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regulatory status, such as via the United States Food and Drug Administration for an investigational new drug to initiate clinical trials on humans, and may include the step of obtaining regulatory approval with a new drug application to market the drug. The entire process—from concept through preclinical testing in the laboratory to clinical trial development, including Phase I–III trials—to approved vaccine or drug typically takes more than a decade. New chemical entity development Broadly, the process of drug development can be divided into preclinical and clinical work. Pre-clinical New chemical entities (NCEs, also known as new molecular entities or NMEs) are compounds that emerge from the process of drug discovery. These h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
