JMC: Chinese scientists have discovered or been able to effectively treat a new drug for chronic obstructive pulmonary disease

December 6, 2020 // -- A recent article in the international magazine Journal of Medicinal Chemistry entitled "Discovery of (S)-2-(1-Amino-3-(3-fluoro-4-methoxyphenyl)-1H-pyrazolo d'pyrimidin-1-yl) propyl)-3-cyclopropyl-5-fluoroquinazolin-4 (3H)-one (IHMT-PI3K-372) as a Potent Selective and PI3K-Essor for The Treatment of Chronic Entive Pulmonary Disease, research report Scientists from the Hefei Institute of Material Sciences of the Chinese Academy of Sciences and others have discovered new inhibitors for the treatment of chronic obstructive pulmonary disease (COPD).
researchers say we have found a potentially selective inhibitor of PI3K, IHMT-PI3K,-372, which may be effective against COPD in in vivo experiments.
photo source: LI FengCOPD is a chronic, reactive respiratory disease characterized by limited respiratory airflow and an abnormally inflammatory reaction to the lungs.
, COPD has become the world's leading health problem and the third leading cause of death.
Although oral PI3K inhibitors, an anti-cancer drug used in clinical practice, are reported to have a variety of adverse side effects, inhalation administration of respiratory diseases may reduce or avoid systemic side effects by transporting the drug directly to the site of action.
in this study, using a fragment hybridization strategy, researchers discovered a new type of PY3K-PI3K-372 inhibitor, IHMT-PI3K-372, which is highly resistant to PI3K gamma, while also showing high selectivity to other type 1 PI3Ks and a relatively low risk of heart toxicity caused by heERG mediatation.
it is worth noting that in the trial of the rodent lung inflammation model, the new inhibitor was able to exhibit high pharmacodynamic properties in drug inhalation and transport, while also improving lung function of the animal model in the subjects.
Finally, the researchers said that the results of this paper confirm that the PI3K inhibitor IHMT-PI3K-372 may be a potential therapeutic candidate for the treatment of chronic obstructive pulmonary disease in the future, although they will need further further research later to analyze the safety and effectiveness of this new inhibitor.
() original source: Feng Li, Xiaofei Liang, Zongru Jiang, et al. Discovery of (S)-2-(1-(4-Amino-3-(3-fluoro-4-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)propyl)-3-cyclopropyl-5-fluoroquinazolin-4(3H)-one (IHMT-PI3Kδ-372) as a Potent and Selective PI3Kδ Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease, Journal of Medicinal Chemistry (2020). DOI: 10.1021/acs.jmedchem.0c01544。