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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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxadiazole
Oxadiazoles are a class of heterocyclic aromatic chemical compound of the azole family; with the molecular formula C2H2N2O. There are four isomers of oxadiazole: File:1,2,3-oxadiazole.svg, 1,2,3-oxadiazole File:1,2,4-oxadiazole.svg, 1,2,4-oxadiazole File:1,2,5-oxadiazole.svg, 1,2,5-oxadiazole(furazan) File:1,3,4-oxadiazole.svg, 1,3,4-oxadiazole 1,2,4-Oxadiazole, 1,2,5-oxadiazole, and 1,3,4-oxadiazole are all known and appear in a variety of pharmaceutical drugs including raltegravir, butalamine, fasiplon, oxolamine, and pleconaril. The 1,2,3-isomer is unstable and ring-opens to form the diazoketone tautomer; however, it does exist within the unusual sydnone motif. In 2018, a compound called bis(1,2,4-oxadiazole)bis(methylene) dinitrate which might have a 1.5 times the power of TNT was developed at the United States Army Research Laboratory (ARL) working with the Los Alamos National Laboratory Los Alamos National Laboratory (often shortened as Los Alamos and LANL) is one o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antibiotic
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting pathogenic bacteria, bacterial infections, and antibiotic medications are widely used in the therapy, treatment and antibiotic prophylaxis, prevention of such infections. They may either bactericide, kill or bacteriostatic agent, 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 language, 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 microorgani ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methicillin-resistant Staphylococcus Aureus
Methicillin-resistant ''Staphylococcus aureus'' (MRSA) is a group of Gram-positive bacteria that are genetically distinct from other strains of ''Staphylococcus aureus''. MRSA is responsible for several difficult-to-treat infections in humans. It caused more than 100,000 deaths attributable to antimicrobial resistance in 2019. MRSA is any strain of ''S. aureus'' that has developed (through natural selection) or acquired (through horizontal gene transfer) a multiple drug resistance to beta-lactam antibiotics. Beta-lactam (β-lactam) antibiotics are a broad-spectrum group that include some penams (penicillin derivatives such as methicillin and oxacillin) and cephems such as the cephalosporins. Strains unable to resist these antibiotics are classified as methicillin-susceptible ''S. aureus'', or MSSA. MRSA is common in hospitals, prisons, and nursing homes, where people with open wounds, invasive devices such as catheters, and weakened immune systems are at greater risk of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clostridium Difficile
''Clostridioides difficile'' (syn. ''Clostridium difficile'') is a bacterium that is well known for causing serious diarrheal infections, and may also cause colon cancer. Also known as ''C. difficile'', or ''C. diff'' (), is Gram-positive species of spore-forming bacteria. ''Clostridioides'' spp. are anaerobic, motile bacteria, ubiquitous in nature and especially prevalent in soil. Its vegetative cells are rod-shaped, pleomorphic, and occur in pairs or short chains. Under the microscope, they appear as long, irregular (often drumstick- or spindle-shaped) cells with a bulge at their terminal ends (forms subterminal spores). Under Gram staining, ''C. difficile'' cells are Gram-positive and show optimum growth on blood agar at human body temperatures in the absence of oxygen. ''C. difficile'' is catalase- and superoxide dismutase-negative, and produces up to three types of toxins: enterotoxin A, cytotoxin B and Clostridioides difficile transferase (CDT). Under stress condition ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxadiazoles
Oxadiazoles are a class of heterocyclic aromatic chemical compound of the azole family; with the molecular formula C2H2N2O. There are four isomers of oxadiazole: File:1,2,3-oxadiazole.svg, 1,2,3-oxadiazole File:1,2,4-oxadiazole.svg, 1,2,4-oxadiazole File:1,2,5-oxadiazole.svg, 1,2,5-oxadiazole(furazan) File:1,3,4-oxadiazole.svg, 1,3,4-oxadiazole 1,2,4-Oxadiazole, 1,2,5-oxadiazole, and 1,3,4-oxadiazole are all known and appear in a variety of pharmaceutical drugs including raltegravir, butalamine, fasiplon, oxolamine, and pleconaril. The 1,2,3-isomer is unstable and ring-opens to form the diazoketone tautomer; however, it does exist within the unusual sydnone motif. In 2018, a compound called bis(1,2,4-oxadiazole)bis(methylene) dinitrate which might have a 1.5 times the power of TNT was developed at the United States Army Research Laboratory (ARL) working with the Los Alamos National Laboratory Los Alamos National Laboratory (often shortened as Los Alamos and LA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
