Article
Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: an fast and atom efficient access to 1-aryl-3-benzylureas.
Bioorganic & medicinal chemistry letters - 15 Sept 2011
Monte Fabio Lo, Kramer Thomas, Boländer Alexander, Plotkin Batya, Eldar-Finkelman Hagit, Fuertes Ana, Dominguez Juan, Schmidt Boris
Abstract excerpt
The glycogen synthase kinase 3 (GSK-3) is implicated in multiple cellular processes and has been linked to the pathogenesis of Alzheimer's disease (AD). In the course of our research topic we synthesized a library of potent GSK-3 inhibitors. We utilized the urea scaffold present in the potent and highly selective GSK-3 inhibitor AR-A014418 (AstraZeneca). This moiety suits both (a) a convergent approach utilizing...
Topics
- Animals
- Chemistry Techniques, Synthetic
- Dose-Response Relationship, Drug
- Glycogen Synthase Kinase 3
- Microwaves
- Models, Molecular
- Molecular Structure
- Phenotype
- Protein Kinase Inhibitors