Publications by authors named "P Ronchi"
The design of inhaled selective phosphatidylinositol 3-kinase delta (PI3Kδ) inhibitors for the treatment of inflammatory lung diseases was pursued. Knowledge-based design of a novel isocoumarin scaffold that was able to adopt a topology ensured the desired PI3Kδ selectivity. Achievement of low nanomolar cellular potencies through hinge binder group optimization, reduction of intrinsic permeability through head group optimization to extend lung retention, and screening of crystalline forms suitable for administration as dry powders culminated in the identification of compound .
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- - Researchers developed new ALK5 inhibitors aimed at treating diseases like cancer and fibrosis, focusing on a specific chemical structure called a 4,6-disubstituted pyridazine core.
- - They used a method called "scaffold-hopping" to explore different chemical frameworks and found a particularly effective compound that was enhanced for inhalation, reducing the risk of side effects.
- - The optimized ALK5 inhibitors demonstrated improved effectiveness and properties for lung retention, suggesting they could be good candidates for creating new inhaled treatment options.
Article Synopsis
- This study investigates the effectiveness of combining vacuum erection devices (VEDs) with PDE5 inhibitors like Tadalafil to improve results after extracorporeal shockwave therapy (ESWT) in men with erectile dysfunction stemming from Peyronie's disease.
- A total of 153 patients were divided into two groups: one received both VEDs and Tadalafil, while the other only received Tadalafil with ESWT.
- Results showed that the group using VEDs experienced significant improvements in penile curvature, pain during erections, and overall erectile function, with effects observed at 3, 6, and 12 months post-treatment.
A selective direct arylation of the different Csp2-H bonds of imidazo[2,1-b]thiazole with (hetero) aryl halides can be achieved simply by switching from a palladium catalyst system to the use of stoichiometric amounts of copper. The observed selectivity, also rationalized by DFT calculations, can be explained by a change in the mechanistic pathways between electrophilic palladation and base-promoted C-H metalation.
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