Spinck, Martin; Bischoff, Matthias; Lampe, Philipp; Meyer-Almes, Franz-Josef; Sievers, Sonja; Neumann, Heinz published an article in 2021. The article was titled 《Discovery of Dihydro-1,4-Benzoxazine Carboxamides as Potent and Highly Selective Inhibitors of Sirtuin-1》, and you may find the article in Journal of Medicinal Chemistry.Product Details of 31106-82-8 The information in the text is summarized as follows:
Sirtuins are signaling hubs orchestrating the cellular response to various stressors with roles in all major civilization diseases. Sirtuins remove acyl groups from lysine residues of proteins, thereby controlling their activity, turnover, and localization. The seven human sirtuins, SirT1-7, are closely related in structure, hindering the development of specific inhibitors. Screening 170,000 compounds, we identify and optimize SirT1-specific benzoxazine inhibitors, Sosbo, which rival the efficiency and surpass the selectivity of selisistat (EX527). The compounds inhibit the deacetylation of p53 in cultured cells, demonstrating their ability to permeate biol. membranes. Kinetic anal. of inhibition and docking studies reveal that the inhibitors bind to a complex of SirT1 and NAD, similar to selisistat. These new SirT1 inhibitors are valuable alternatives to selisistat in biochem. and cell biol. studies. Their greater selectivity may allow the development of better targeted drugs to combat SirT1 activity in diseases such as cancer, Huntington’s chorea, or anorexia. In the part of experimental materials, we found many familiar compounds, such as 2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8Product Details of 31106-82-8)
2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8) belongs to pyridine. Pyridines form stable salts with strong acids. Pyridine itself is often used to neutralize acid formed in a reaction and as a basic solvent. Product Details of 31106-82-8