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Uses and synthesis methods of Zileuton:Asthma is a common chronic disease, accounting for about 10% in developed countries, and its morbidity and disability rates are increasing globally. Asthma has caused widespread concern around the world.
In the late 1980s, asthma was recognized as a chronic inflammatory disease characterized by airway hyperresponsiveness and reversible airway obstruction. With the deepening of the research on the mechanism of airway inflammation in asthma, the development of anti-inflammatory therapy including specific medium antagonists has become a hot topic in the management of asthma prevention and treatment.
Among the current anti-asthma drugs,β2 agonists can rapidly suppress symptoms, but clinical application has found that agonists are associated with increased mortality of asthma, and rebound phenomenon after drug withdrawal and the possibility of aggravating asthma conditions.
Theophylline preparation has a narrow therapeutic window and greater toxicity and side effects. The efficacy of corticosteroid is definite, but the anti-inflammatory effect is non-specific and the adverse reactions are many.
It is still necessary to develop new efficient and safe drugs for asthma treatment. The research on lipid antagonists and inhibitors is a new approach for asthma treatment.
Zileuton English alias:
(+) - N - hydroxy - N - (1 - benzo [b] thien - 2 - ylethyl) urea. Zileuton; Leutrol; 1 - (N - hydroxy - N - {benzo [b] thien - 2 - yl) baton rouge} urea; 1 - (1 - benzo [b] thien - 2 - ylethyl) - 1 - hydroxyurea; 1-(1-(Benzo[b]thiophen-2-yl)ethyl)-1-hydroxyurea;
Production method:
2-acetyl benzothiophene was dissolved in pyridine-ethanol solution, hydroxylamine hydrochloride was added and reacted at room temperature. Hydroxylamine was reduced by adding meborane - pyridine complex to the ethanol solution of the reaction product, and then adding hydrogen chloride ethanol solution. Hydroxylamine added trimethylsilyl isocyanate to dioxane ring and heated to get the eluent. Or the above hydroxylamine and potassium fluoride and hydrochloric acid aqueous solution, also can obtain Zileuton.
Use of Zileuton Pass:
Anti-leukotriene drugs. It is used to treat asthma by reducing the production of leukotrienes by inhibiting 5-lipoxyase.
Zileuton is a new leukotriene antagonist. Zileuton inhibits the catalytic conversion of arachidonic acid to leukotriene by inhibiting the activity of 5-lipoxygenase. Leukotriene is known to be an important factor in asthma among many inflammatory mediators.
Therefore, this product is clinically used for the prevention and maintenance of chronic asthma in adults and adolescents over the age of 12. In addition, this product can prophylactically reduce aspirin-induced bronchospasm in asthmatic patients with aspirin sensitivity and airway hypersensitivity (constriction) caused by cold air and exercise.
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