874-69-1Relevant articles and documents
5-Imino-1,2,4-thiadiazoles: First small molecules As substrate competitive inhibitors of glycogen synthase kinase 3
Palomo, Valle,Perez, Daniel I.,Perez, Concepcion,Morales-Garcia, Jose A.,Soteras, Ignacio,Alonso-Gil, Sandra,Encinas, Arantxa,Castro, Ana,Campillo, Nuria E.,Perez-Castillo, Ana,Gil, Carmen,Martinez, Ana
, p. 1645 - 1661 (2012)
Cumulative evidence strongly supports that glycogen synthase kinase-3 (GSK-3) is a pathogenic molecule when it is up-dysregulated, emerging as an important therapeutic target in severe unmet human diseases. GSK-3 specific inhibitors might be promising effective drugs for the treatment of devastating pathologies such as neurodegenerative diseases, stroke, and mood disorders. As GSK-3 has the ability to phosphorylate primed substrates, small molecules able to bind to this site should be perfect drug candidates, able to partially block the activity of the enzyme over some specific substrates. Here, we report substituted 5-imino-1,2,4-thiadiazoles as the first small molecules able to inhibit GSK-3 in a substrate competitive manner. These compounds are cell permeable, able to decrease inflammatory activation and to selectively differentiate neural stem cells. Overall, 5-imino-1,2,4-thiadiazoles are presented here as new molecules able to decrease neuronal cell death and to increase endogenous neurogenesis blocking the GSK-3 substrate site
Conformational Studies by Dynamic Nuclear Magnetic Resonance. Part 17. Stereodynamic Processes in Hindered Piperidyl-amides and -amidines
Lunazzi, Lodovico,Macciantelli, Dante,Tassi, Danilo,Dondoni, Alessandro
, p. 717 - 723 (2007/10/02)
It has been shown that molecules containing hindered piperidyl rings can have planar or perpendicular conformations depending on the functional group attached to nitrogen.In addition, we have shown that when the group is CR=NPh (amidines) the molecule may
