Halofuginone (CAS NO: 55837-20-2), also known as man-one halogen, bromine chloride piperaquine ketone. Chemical name 7 - bromo 6 - chloro -3 - [3 - [(2R, 3S) -3 - hydroxy -2 - piperidinyl] -2 - oxo-propyl] -4 (3H) - quinazolinone . Room temperature as white or light gray crystalline powder, odorless, bitter taste.Halofuginone not only as a special type I collagen synthesis inhibitor, has begun to be applied clinically, but also as an inhibitor of tumor growth and metastasis. The anticancer mechanism of ketone can inhibit collagen Changshan overproduction, which can inhibit tumor growth in a range of essential cellular activity, including angiogenesis, cell proliferation and migration.There is no domestic industrial production Changshan ketone products rely mainly on imported and expensive, therefore, to find a suitable synthetic route of industrialization, the product will be very good prospects. The technology to 3 - hydroxypyridine as raw materials, ammonia methylation and diethylamine, formaldehyde reaction, the resulting compounds by acetylation, bromination, 3-hydroxy protection after lithium, acetonitrile reaction, hydrolysis under acidic conditions , hydrogenation, to be intermediate, then α-carboxyl group such as bromo ketone Changshan generated.
Halofuginone is a coccidiostat employed inwards veterinary surgeon medicament. It's a man-made halogenated derived function by febrifugine, a innate quinazolinone alkaloid which could constitute came up inward the Formosan herbaceous plant Dichroa febrifuga (Yangtze Shan).Collgard Biopharmaceuticals constitutes breaking halofuginone because the discourse from dermatosclerosis and it's encountered orphaned do drugs appellation from the U.S. government. FDA.
Halofuginone stamps down the evolution oftentimes benefactor seventeen cellphones, exempt cellphones that bet an crucial instrumentalists in autoimmune disorder, merely them arranges not dissemble extra kinds of liothyronine cells which Byzantine inwards pattern insusceptible mathematical function. Halofuginone so consumes potential difference because the discourse of autoimmune disorders.Halofuginine institutes as easily an inhibitor from collagen typecast I cistron formula and since a issue it could suppress tumor electric cell increase.Halofuginone is a coccidiostat for young chickens and young turkeys. In higher doses, halofuginone is a growth depressant, impairs feed utilization, and reduces feed intake. In rats it causes alopecia. The compound is prohibited from use during the last four days before slaughter ( withdrawalperiod). Halofuginone is extracted from enzyme-digested chicken liver as a free base into ethyl acetate and partitioned into ammonium acetate buffer solution.The halofuginone is concentrated with Sep-Pak CIS cartridges and eluted with methyl alcohol. The eluant is evaporated to dryness and the residue dissolved in the HPLC mobile phase. Analysis is achieved by HPLC using a BONDAPAK C,, column and a variable wavelength UV detector.Pharmacological effectsChangshan ketone Changshan from medicinal plants in advance out of an alkaloid, has been able to synthetic, broad-spectrum anticoccidial for new drugs. Major role in the first-and second-generation schizonts. 6 of chicken Eimeria and 2 of the most damaging in turkeys Eimeria have a strong inhibitory effect. Eimeria of rabbits also have some effect. Mixed feeding, every 1000kg feed 500g.
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