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Ravuconazole
Ravuconazole (codenamed BMS-207147 and ER-30346) is a potent triazole antifungal, the development of which was discontinued in 2007. The drug has shown to have a similar spectrum of activity to voriconazole, with an increased half-life. However, ravuconazole has limited activity against species of ''Fusarium'', '' Scedosporium'', and ''Zygomycetes''. See also * Albaconazole * Fosravuconazole Fosravuconazole (trade name Nailin) is a triazole antifungal agent. In Japan, it is approved for the treatment of onychomycosis, a fungal infection of the nail. It is a prodrug that is converted into ravuconazole. Drugs for Neglected Dise ..., a prodrug of ravuconazole * Isavuconazole References External links * 27-Hydroxylase inhibitors Lanosterol 14α-demethylase inhibitors Nitriles Fluoroarenes Phenylethanolamines Tertiary alcohols Thiazoles Triazole antifungals Abandoned drugs {{antiinfective-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antifungal
An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually obtained by a doctor's prescription, but a few are available over the counter (OTC). The evolution of antifungal resistance is a growing threat to health globally. Routes of administration Ocular Indicated when the fungal infection is located in the eye. There is currently only one ocular antifungal available: natamycin. However, various other antifungal agents could be compounded in this formulation. Intrathecal Used occasionally when there's an infection of the central nervous system and other systemic options cannot reach the concentration required in that region for therapeutic benefit. Example(s): amphotericin B. Vaginal This may be used to treat some fungal in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fosravuconazole
Fosravuconazole (trade name Nailin) is a triazole antifungal agent. In Japan, it is approved for the treatment of onychomycosis, a fungal infection of the nail. It is a prodrug that is converted into ravuconazole. Drugs for Neglected Diseases Initiative (DNDi) and the Japanese pharmaceutical company Eisai found that fosravuconazole works as a treatment for mycetoma, a serious condition. The Phase II clinical trial found that oral fosravuconazole was safe, patient-friendly, and effective in treating eumycetoma. Eumycetoma mainly affects young adults in poorer, rural areas; the standard treatment is itraconazole, which is much more expensive at about US$ The United States dollar (Currency symbol, symbol: Dollar sign, $; ISO 4217, currency code: USD) is the official currency of the United States and International use of the U.S. dollar, several other countries. The Coinage Act of 1792 introdu ...2,000 for a year than fosravuconazole and unaffordable, and not availabl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Triazole
A triazole is a heterocyclic compound featuring a five-membered ring of two carbon atoms and three nitrogen atoms with molecular formula C2H3N3. Triazoles exhibit substantial Isomer, isomerism, depending on the positioning of the nitrogen atoms within the ring. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. However, triazoles are also useful in bioorthogonal chemistry, because the large number of nitrogen atoms causes triazoles to react similar to Azide, azides. Lastly, the many free lone pairs in triazoles make them useful as coordination compounds, although not typically as Piano stool complex, haptic ligands. Isomerism There are four triazole isomers, which are conventionally divided into two pairs of Tautomer, tautomers. In the 1,2,3-Triazole, 1,2,3-triazoles, the three nitrogen atoms are adjacent; in the 1,2,4-Triazole, 1,2,4-triazoles, an interstitial carbon separates out one nitrogen atom. Each category ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lanosterol 14α-demethylase Inhibitors
Lanosterol is a tetracyclic triterpenoid and is the compound from which all animal and fungal steroids are derived. By contrast, plant steroids are produced via cycloartenol. In the eyes of vertebrates, lanosterol is a natural constituent, having a role in maintaining health of the lens. Lanosterol is the precursor to cholesterol. Biosynthesis The biosynthesis of lanosterol has been intensively investigated. Elaboration of lanosterol under enzyme catalysis leads to other steroids. 14-Demethylation of lanosterol by CYP51 eventually yields cholesterol. Research as an eye drop supplement As a molecule naturally enriched in the eye lens, lanosterol is a component involved in maintenance of lens clarity. Its proposed mechanism of action is to inhibit the aggregation of crystallin proteins, which contribute to the clouding of vision by forming cataracts. Lanosterol is under research for its potential as a therapeutic additive in eye drops to inhibit the aggregation of crystallin p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thiazoles
Thiazole (), or 1,3-thiazole, is a 5-membered heterocyclic compound that contains both sulfur and nitrogen. The term 'thiazole' also refers to a large family of derivatives. Thiazole itself is a pale yellow liquid with a pyridine-like odor and the molecular formula C3H3NS. The thiazole ring is notable as a component of the vitamin thiamine (B1). Molecular and electronic structure Thiazoles are members of the azoles, heterocycles that include imidazoles and oxazoles. Thiazole can also be considered a functional group when part of a larger molecule. Being planar thiazoles are characterized by significant pi-electron delocalization and have some degree of aromaticity, more so than the corresponding oxazoles. This aromaticity is evidenced by the 1H NMR chemical shift of the ring protons, which absorb between 7.27 and 8.77 ppm, indicating a strong diamagnetic ring current. The calculated pi-electron density marks C5 as the primary site for electrophilic substitution, and C2-H a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tertiary Alcohols
In chemistry, an alcohol (), is a type of organic compound that carries at least one hydroxyl () functional group bound to a Saturated and unsaturated compounds, saturated carbon atom. Alcohols range from the simple, like methanol and ethanol, to complex, like sugar alcohols and cholesterol. The presence of an OH group strongly modifies the properties of Hydrocarbon, hydrocarbons, conferring Hydrophile, hydrophilic (water-loving) properties. The OH group provides a site at which many reactions can occur. History The flammable nature of the exhalations of wine was already known to ancient natural philosophers such as Aristotle (384–322 BCE), Theophrastus (–287 BCE), and Pliny the Elder (23/24–79 CE). However, this did not immediately lead to the isolation of alcohol, even despite the development of more advanced distillation techniques in second- and third-century Roman Egypt. An important recognition, first found in one of the writings attributed to Jabir ibn Hayyan, J� ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenylethanolamines
Phenylethanolamine (sometimes abbreviated PEOH), or β-hydroxyphenethylamine, is a trace amine with a structure similar to those of other trace phenethylamines as well as the catecholamine neurotransmitters dopamine, norepinephrine, and epinephrine. As an organic compound, phenylethanolamine is a β-hydroxylated phenethylamine that is also structurally related to a number of synthetic drugs in the substituted phenethylamine class. In common with these compounds, phenylethanolamine has strong cardiovascular activity and, under the name ''Apophedrin'', has been used as a drug to produce topical vasoconstriction.''The Merck Index, 10th Ed.'' (1983), p. 1051, Merck & Co., Rahway. In appearance, phenylethanolamine is a white solid. Phenylethanolamine is perhaps best known in the field of bioscience as part of the enzyme name " phenylethanolamine N-methyl transferase", referring to an enzyme which is responsible for the conversion of norepinephrine into epinephrine, as well as other r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluoroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitriles
In organic chemistry, a nitrile is any organic compound that has a functional group. The name of the compound is composed of a base, which includes the carbon of the , suffixed with "nitrile", so for example is called "propionitrile" (or propanenitrile). The prefix ''cyano-'' is used interchangeably with the term ''nitrile'' in industrial literature. Nitriles are found in many useful compounds, including methyl cyanoacrylate, used in super glue, and nitrile rubber, a nitrile-containing polymer used in latex, latex-free laboratory and medical gloves. Nitrile rubber is also widely used as automotive and other seals since it is resistant to fuels and oils. Organic compounds containing multiple nitrile groups are known as cyanocarbons. Inorganic compounds containing the group are not called nitriles, but cyanides instead. Though both nitriles and cyanides can be derived from cyanide salts, most nitriles are not nearly as toxic. Structure and basic properties The N−C−C geome ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isavuconazole
Isavuconazonium, sold under the brand name Cresemba, is a systemic antifungal medication of the triazole class which is used to treat invasive aspergillosis and mucormycosis. It is used as the sulfate. It is taken by mouth or given via injection into a vein. The most common side effects include abnormal liver enzyme tests, nausea, vomiting, difficulty breathing, abdominal pain, diarrhea, injection site reactions, headache, low blood potassium, and skin rash. Isavuconazonium is a prodrug of isavuconazole. Medical uses Isavuconazonium is used to treat invasive aspergillosis and invasive mucormycosis in adults aged eighteen years and older. It is available in a capsule for administration by mouth and as a powder for administration via infusion. Contraindications Isavuconazonium is contraindicated in people taking strong CYP3A4 inhibitors, strong CYP3A4 inducers, or moderate CYP3A4 or CYP3A5 inducers. It is contraindicated in people with familial short QT syndrome. Side effe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Albaconazole
Albaconazole (development code UR-9825) is an experimental triazole antifungal. It has potential broad-spectrum activity. The drug blocks a number of CYP450 liver enzymes. It has also been studied as an antiprotozoal Antiprotozoal agents ( ATC code: ATC P01) is a class of pharmaceuticals used in treatment of protozoan infection. A paraphyletic group, protozoans have little in common with each other. For example, '' Entamoeba histolytica'', a unikont eukary ... agent. References Chloroarenes Fluoroarenes Lactams Lanosterol 14α-demethylase inhibitors Phenylethanolamines Quinazolines Tertiary alcohols Triazole antifungals {{antiinfective-agent-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
