Related Products of 19759-66-1. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile
Glycogen synthase kinase 3 (GSK-3)has become known for its multifactorial involvement in the pathogenesis of Alzheimer’s disease. In this study, a benzothiazole- and benzimidazole set of 1-aryl-3-(4-methoxybenzyl)ureas were synthesised as proposed Cys199-targeted covalent inhibitors of GSK-3beta, through the incorporation of an electrophilic warhead onto their ring scaffolds. The nitrile-substituted benzimidazolylurea 2b (IC50 = 0.086 ¡À 0.023 muM)and halomethylketone-substituted benzimidazolylurea 9b (IC50 = 0.13 ¡À 0.060 muM)displayed high GSK-3beta inhibitory activity, in comparison to reference inhibitor AR-A014418 (1, IC50 = 0.072 ¡À 0.043)in our assay. The results suggest further investigation of 2b and 9b as potential covalent inhibitors of GSK-3beta, since a targeted interaction might provide improved kinase-selectivity.
Glycogen synthase kinase 3 (GSK-3)has become known for its multifactorial involvement in the pathogenesis of Alzheimer’s disease. In this study, a benzothiazole- and benzimidazole set of 1-aryl-3-(4-methoxybenzyl)ureas were synthesised as proposed Cys199-targeted covalent inhibitors of GSK-3beta, through the incorporation of an electrophilic warhead onto their ring scaffolds. The nitrile-substituted benzimidazolylurea 2b (IC50 = 0.086 ¡À 0.023 muM)and halomethylketone-substituted benzimidazolylurea 9b (IC50 = 0.13 ¡À 0.060 muM)displayed high GSK-3beta inhibitory activity, in comparison to reference inhibitor AR-A014418 (1, IC50 = 0.072 ¡À 0.043)in our assay. The results suggest further investigation of 2b and 9b as potential covalent inhibitors of GSK-3beta, since a targeted interaction might provide improved kinase-selectivity.
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Reference£º
Thiazole | C3H2253NS – PubChem,
Thiazole | chemical compound | Britannica