1429014-07-2

Upstream product

• 100-39-0 benzyl bromide 
• 40928-13-0 4-chloroisatoic anhydride 
• 35709-36-5 4-chloro-N-benzylisatoic anhydride 
• 105-53-3 diethyl malonate 

Downstream Products

• 1429014-27-6 1-benzyl-7-chloro-N'-dodecanoyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbohydrazide 
• 1429014-26-5 1-benzyl-7-chloro-4-hydroxy-N'-octanoyl-2-oxo-1,2-dihydroquinoline-3-carbohydrazide 

Relevant academic research and scientific papers

Subtly Modulating Glycogen Synthase Kinase 3 β: Allosteric Inhibitor Development and Their Potential for the Treatment of Chronic Diseases

Glycogen synthase kinase 3 β (GSK-3β) is a central target in several unmet diseases. To increase the specificity of GSK-3β inhibitors in chronic treatments, we developed small molecules allowing subtle modulation of GSK-3β activity. Design synthesis, structure-Activity relationships, and binding mode of quinoline-3-carbohydrazide derivatives as allosteric modulators of GSK-3β are presented here. Furthermore, we show how allosteric binders may overcome the β-catenin side effects associated with strong GSK-3β inhibition. The therapeutic potential of some of these modulators has been tested in human samples from patients with congenital myotonic dystrophy type 1 (CDM1) and spinal muscular atrophy (SMA) patients. We found that compound 53 improves delayed myogenesis in CDM1 myoblasts, while compounds 1 and 53 have neuroprotective properties in SMA-derived cells. These findings suggest that the allosteric modulators of GSK-3β may be used for future development of drugs for DM1, SMA, and other chronic diseases where GSK-3β inhibition exhibits therapeutic effects.

Heterocyclic GSK-3 Allosteric Modulators

The present invention relates to heterocyclic substituted quinoline derivatives as allosteric inhibitors of the glycogen synthase kinase-3 (GSK-3) enzyme. Therefore, these compounds are useful for the manufacturing of a medicament designed for the treatme

HETEROCYCLIC GSK-3 ALLOSTERIC MODULATORS

The invention relates to heterocyclic derivatives of substituted quinolines as allosteric inhibitors of the glycogen synthase kinase 3 (GSK-3) enzyme. Thus, said compounds can be used in the production of a drug for the treatment and/or prevention of diseases in which GSK-3 is involved, such as: neurodegenerative diseases, inflammatory diseases, cancer and diabetes, as well as to promote a plurality of regenerative processes..