Effective suppression of respiratory inflammatory response Slow-blocking lung pilot compounds were found

Chronic obstructive pulmonary disease (COPD) is a respiratory disease characterized by persistent air flow restriction, characterized by emphysema, airway fibrosis and chronic bronchitis.
recent years, joulmonary retardation has become the world's third leading cause of death, leading to millions of deaths each year, and high morbidity and fatality rates have made it a global health problem.
At present, the treatment of ADHD is mainly dependent on bronchial dilation agents, i.e. regulatory drugs for smooth muscle cells, which can reduce ADHD lung symptoms and the frequency of seizures, but can not prevent and reverse the gradual loss of lung function.
the treatment of chronic inflammation of the respiratory tract, which is mainly manifested as complex respiratory inflammation, is the most direct treatment.
previous studies have shown that lipid kinase PI3K, expressed mainly in white blood cells, is closely related to respiratory inflammation.
how to develop safe and efficient PI3K inhibitors to meet the growing clinical demand has become a challenge for researchers.
Liu Qingsong and Liu Jing team of researchers based on the marketed drug research, combined with computer-aided drug design methods, using fragment hybridization combination strategy, and through enzymatic activity detection and selective evaluation, found the pilot compound IHMT-PI3K-372.
inhibitors showed high activity and selectivity at the protein and cellular levels, and also showed good selectivity in the kinase group.
addition, the compound does not cause potential heart toxicity and is suitable for inhalation.
studies have shown that inhalation of administration for respiratory diseases may reduce the dose of drug use and provide direct access to lesions, thereby reducing or avoiding systemic toxic side effects caused by the drug.
in rats, IHMT-PI3K-372 improved lung function in rats by atomized inhalation.
preclinical safety evaluation, pharmacodynamics research, and pharmacological studies have shown that IHMT-PI3K-372 may be a preclinical candidate for the treatment of slow-blocking lungs.
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