I found the field of Pharmacology & Pharmacy very interesting. Saw the article Synthesis of Coumarin Derivatives as Versatile Scaffolds for GSK-3 beta Enzyme Inhibition published in 2020.0. Safety of m-Methoxyphenol, Reprint Addresses Lacerda, V (corresponding author), Univ Fed Espirito Santo, Ctr Ciencias Exatas, Dept Quim, Av Fernando Ferrari 514, BR-29075910 Vitoria, ES, Brazil.. The CAS is 150-19-6. Through research, I have a further understanding and discovery of m-Methoxyphenol
Background: Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer’s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3 beta isoforms is likely to represent an effective strategy against AD. Objective: The present work aimed to design and synthesize coumarin derivatives to explore their potential as GSK-3 beta kinase inhibitors. Methods: The through different synthetic methods were used to prepare coumarin derivatives. The GSK-3 beta activity was measured through the ADP-Glo (TM) Kinase Assay, which quantifies the kinase-dependent enzymatic production of ADP from ATP, using a coupled-luminescence-based reaction. A docking study was performed by using the crystallographic structure of the staurosporine/GSK-3 beta complex [Protein Data Bank (PDB) code: 1Q3D]. Results: The eleven coumarin derivatives were obtained and evaluated as potential GSK-3 beta inhibitors. Additionally, in silico studies were performed. The results revealed that the compounds 5c, 5d, and 6b inhibited GSK-3 beta enzymatic activity by 38.97-49.62% at 1 mM. The other coumarin derivatives were tested at 1 mM, 1 mu M, and 1 nM concentrations and were shown to be inhibitor candidates, with significant IC50 (1.224-6.875 mu M) values, except for compound 7c (IC50 – 10.809 mu M). Docking simulations showed polar interactions between compound 5b and Lys(85) and Ser(203), clarifying the mechanism of the most potent activity. Conclusion: The coumarin derivatives 3a and 5b, developed in this study, showed remarkable activity as GSK-3 beta inhibitors.
About m-Methoxyphenol, If you have any questions, you can contact Francisco, CS; Javarini, CL; Barcelos, ID; Morais, PAB; de Paula, H; Borges, WD; Neto, AC; Lacerda, V or concate me.. Safety of m-Methoxyphenol
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles