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Cadazolid
Cadazolid is an experimental antibiotic of the oxazolidinone class made by Actelion Pharmaceuticals Ltd. which is effective against ''Clostridium difficile'', a major cause of drug resistant diarrhea in the elderly. Current drug treatments for this infection involve orally delivered antibiotics, principally fidaxomicin, metronidazole and vancomycin; the last two drugs are the principal therapeutic agents in use, but fail in approximately 20 to 45% of the cases. The drug works by inhibiting synthesis of proteins in the bacteria, thus inhibiting the production of toxins and the formation of spores. Cadazolid progressed through to Phase III clinical trials, but in its financial results for Q1 2018, Idorsia mentions that Actelion informed them that "following completion of Phase 3 data analysis of cadazolid - it has decided to discontinue the development of the compound." __TOC__ Structure The chemical structure of cadazolid combines the pharmacophores of oxazolidinone and fluoroq ...
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Actelion
Actelion is a pharmaceuticals and biotechnology company established in December 1997, headquartered in Allschwil near Basel, Switzerland. Actelion focuses on the manufacture of drugs that treat rare diseases and orphan diseases. Some of the drugs it has produced have been used to treat patients with symptoms related to central nervous system disorders, irregular heart conditions, immune system disorders and cancer. One of the focuses of Actelion is treating individuals with pulmonary arterial hypertension (PAH), a heart condition that leaves patients with a short life expectancy (7–9 years) even with treatment. Actelion scientists were among the first to work in the field of endothelian receptor antagonists. Actelion was initially financed with venture capital provided through a syndicate including Atlas Venture, Sofinnova and HealthCap. Actelion develops and sells drugs in the continents of Asia, Europe and North and South America. Actelion has 29 operative affiliate ...
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Surotomycin
Surotomycin was an investigational oral antibiotic. This macrolide antibiotic was under investigation by Merck & Co (who acquired Cubist Pharmaceuticals) for the treatment of life-threatening diarrhea, commonly caused by the bacterium ''Clostridium difficile''. After reaching phase III in clinical trials, its production was discontinued in 2017 due to its non-superiority to current therapies. See also * Cadazolid * Fidaxomicin * Ridinilazole * SCHEMBL19952957 SCHEMBL19952957 is an oxadiazole based antibiotic, originally developed in 2014 as a potential treatment for infections with methicillin-resistant ''Staphylococcus aureus'' (MRSA) and other antibiotic resistant bacteria. Subsequently, it has bee ... References Antibiotics Macrolides {{antibiotic-stub ...
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SCHEMBL19952957
SCHEMBL19952957 is an oxadiazole based antibiotic, originally developed in 2014 as a potential treatment for infections with methicillin-resistant ''Staphylococcus aureus'' (MRSA) and other antibiotic resistant bacteria. Subsequently, it has been found to be useful against ''Clostridium difficile'' as it not only kills active bacteria, but also inhibits the germination of the dormant spores which can otherwise often lead to persistent infections that repeatedly recur upon cessation of antibiotic treatment. While it is still only being researched in animals at this stage, this dual action is a significant advance over existing antibiotics, and it is likely that drugs from this class may be developed as new medications for the treatment of antibiotic resistant infections in humans. See also * Cadazolid * Fidaxomicin * Ridinilazole Ridinilazole (previously known as SMT19969) is an investigational small molecule antibiotic being evaluated for oral administration to treat ''Clos ...
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Antibacterial
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of such infections. They may either kill or inhibit the growth of bacteria. A limited number of antibiotics also possess antiprotozoal activity. Antibiotics are not effective against viruses such as the common cold or influenza; drugs which inhibit viruses are termed antiviral drugs or antivirals rather than antibiotics. Sometimes, the term ''antibiotic''—literally "opposing life", from the Greek roots ἀντι ''anti'', "against" and βίος ''bios'', "life"—is broadly used to refer to any substance used against microbes, but in the usual medical usage, antibiotics (such as penicillin) are those produced naturally (by one microorganism fighting another), whereas non-antibiotic antibacterials (such as sulfonamides and anti ...
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Fluoroquinolone
A quinolone antibiotic is a member of a large group of broad-spectrum bacteriocidals that share a bicyclic core structure related to the substance 4-quinolone. They are used in human and veterinary medicine to treat bacterial infections, as well as in animal husbandry, specifically poultry production. Nearly all quinolone antibiotics in use are fluoroquinolones, which contain a fluorine atom in their chemical structure and are effective against both Gram-negative and Gram-positive bacteria. One example is ciprofloxacin, one of the most widely used antibiotics worldwide. Medical uses Fluoroquinolones are often used for genitourinary infections and are widely used in the treatment of hospital-acquired infections associated with urinary catheters. In community-acquired infections, they are recommended only when risk factors for multidrug resistance are present or after other antibiotic regimens have failed. However, for serious acute cases of pyelonephritis or bacterial ...
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Ridinilazole
Ridinilazole (previously known as SMT19969) is an investigational small molecule antibiotic being evaluated for oral administration to treat ''Clostridioides difficile'' infection (CDI). In vitro, it is bactericidal against ''C. difficile'' and suppresses bacterial toxin production; the mechanism of action is thought to involve inhibition of cell division. It has properties which are desirable for the treatment of CDI, namely that it is a narrow-spectrum antibiotic which exhibits activity against ''C. difficile'' while having little impact on other normal intestinal flora and that it is only minimally absorbed systemically after oral administration. At the time ridinilazole was developed, there were only three antibiotics in use for treating CDI: vancomycin, fidaxomicin, and metronidazole. The recurrence rate of CDI is high, which has spurred research into other treatment options with the aim to reduce the rate of recurrence. , two phase II trials have been completed and two phas ...
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Fidaxomicin
Fidaxomicin, sold under the brand name Dificid among others, is the first member of a class of narrow spectrum macrocyclic antibiotic drugs called tiacumicins. It is a fermentation product obtained from the actinomycete '' Dactylosporangium aurantiacum'' subspecies ''hamdenesis''. Fidaxomicin is minimally absorbed into the bloodstream when taken orally, is bactericidal, and selectively eradicates pathogenic '' Clostridioides difficile'' with relatively little disruption to the multiple species of bacteria that make up the normal, healthy intestinal microbiota. The maintenance of normal physiological conditions in the colon may reduce the probability of recurrence of ''Clostridioides difficile'' infection. It is marketed by Merck, which acquired Cubist Pharmaceuticals in 2015, and had in turn bought the originating company, Optimer Pharmaceuticals. It is used for the treatment of ''Clostridioides difficile'' infection, which is also known as ''Clostridioides difficile''-ass ...
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Colon (anatomy)
The large intestine, also known as the large bowel, is the last part of the gastrointestinal tract and of the digestive system in tetrapods. Water is absorbed here and the remaining waste material is stored in the rectum as feces before being removed by defecation. The colon is the longest portion of the large intestine, and the terms are often used interchangeably but most sources define the large intestine as the combination of the cecum, colon, rectum, and anal canal. Some other sources exclude the anal canal. In humans, the large intestine begins in the right iliac region of the pelvis, just at or below the waist, where it is joined to the end of the small intestine at the cecum, via the ileocecal valve. It then continues as the colon ascending the abdomen, across the width of the abdominal cavity as the transverse colon, and then descending to the rectum and its endpoint at the anal canal. Overall, in humans, the large intestine is about long, which is about one-fi ...
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Sweden
Sweden, ; fi, Ruotsi; fit, Ruotti; se, Ruoŧŧa; smj, Svierik; sje, Sverji; sju, Sverje; sma, Sveerje or ; yi, שוועדן, Shvedn; rmu, Svedikko; rmf, Sveittiko. formally the Kingdom of Sweden, is a Nordic countries, Nordic country located on the Scandinavian Peninsula in Northern Europe. It borders Norway to the west and north, and Finland to the east. At , Sweden is the largest Nordic country and the List of European countries by area, fifth-largest country in Europe. The Capital city, capital and largest city is Stockholm. Sweden has a population of 10.5 million, and a low population density of ; around 87% of Swedes reside in urban areas in the central and southern half of the country. Sweden’s urban areas together cover 1.5% of its land area. Because the country is so long, ranging from 55th parallel north, 55°N to 69th parallel north, 69°N, the climate of Sweden is diverse. Sweden has been inhabited since Prehistoric Sweden, prehistoric times, . T ...
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In Vitro
''In vitro'' (meaning in glass, or ''in the glass'') studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in biology and its subdisciplines are traditionally done in labware such as test tubes, flasks, Petri dishes, and microtiter plates. Studies conducted using components of an organism that have been isolated from their usual biological surroundings permit a more detailed or more convenient analysis than can be done with whole organisms; however, results obtained from ''in vitro'' experiments may not fully or accurately predict the effects on a whole organism. In contrast to ''in vitro'' experiments, '' in vivo'' studies are those conducted in living organisms, including humans, and whole plants. Definition ''In vitro'' ( la, in glass; often not italicized in English usage) studies are conducted using components of an organism that have been isolated f ...
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Chemical Structure
A chemical structure determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid. Molecular geometry refers to the spatial arrangement of atoms in a molecule and the chemical bonds that hold the atoms together, and can be represented using structural formulae and by molecular models; complete electronic structure descriptions include specifying the occupation of a molecule's molecular orbitals. Structure determination can be applied to a range of targets from very simple molecules (e.g., diatomic oxygen or nitrogen), to very complex ones (e.g., such as protein or DNA). Background Theories of chemical structure were first developed by August Kekulé, Archibald Scott Couper, and Aleksandr Butlerov, among others, from about 1858. These theories were first to state that chemical compounds are not a random cluster of atoms and functional groups, but rather had a definite o ...
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Pharmacophore
300px, An example of a pharmacophore model. A pharmacophore is an abstract description of molecular features that are necessary for molecular recognition of a ligand by a biological macromolecule. IUPAC defines a pharmacophore to be "an ensemble of steric and electronic features that is necessary to ensure the optimal supramolecular interactions with a specific biological target and to trigger (or block) its biological response". A pharmacophore model explains how structurally diverse ligands can bind to a common receptor site. Furthermore, pharmacophore models can be used to identify through de novo design or virtual screening novel ligands that will bind to the same receptor. Features Typical pharmacophore features include hydrophobic centroids, aromatic rings, hydrogen bond acceptors or donors, cations, and anions. These pharmacophoric points may be located on the ligand itself or may be projected points presumed to be located in the receptor. The features need to match ...
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