Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. 166591-85-1, C15H19NO4. A document type is Article, introducing its new discovery., 166591-85-1
Pyridinylimidazoles as dual glycogen synthase kinase 3beta/p38alpha mitogen-activated protein kinase inhibitors
Compounds simultaneously inhibiting two targets that are involved in the progression of the same complex disease may exhibit additive or even synergistic therapeutic effects. Here we unveil 2,4,5-trisubstituted imidazoles as dual inhibitors of p38alpha mitogen-activated protein kinase and glycogen synthase kinase 3beta (GSK3beta). Both enzymes are potential therapeutic targets for neurodegenerative disorders, like Alzheimer’s disease. A set of 39 compounds was synthesized and evaluated in kinase activity assays for their ability to inhibit both target kinases. Among the synthesized compounds, potent dual-target-directed inhibitors showing IC50 values down to the low double-digit nanomolar range, were identified. One of the best balanced dual inhibitors presented in here is N-(4-(2-ethyl-4-(4-fluorophenyl)-1H-imidazol-5-yl)pyridin-2-yl)cyclopropanecarboxamide (20c) (p38alpha, IC50 = 16 nM; GSK3beta, IC50 = 35 nM) featuring an excellent metabolic stability and an appreciable isoform selectivity over the closely related GSK3alpha. Our findings were rationalized by computational docking studies based on previously published X-ray structures.
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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem