Recommanded Product: 89466-08-0In 2019 ,《Pyridinylimidazoles as GSK3β Inhibitors: The Impact of Tautomerism on Compound Activity via Water Networks》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Heider, Fabian; Pantsar, Tatu; Kudolo, Mark; Ansideri, Francesco; De Simone, Angela; Pruccoli, Letizia; Schneider, Taiane; Goettert, Marcia Ines; Tarozzi, Andrea; Andrisano, Vincenza; Laufer, Stefan A.; Koch, Pierre. The article conveys some information:
Glycogen synthase kinase-3β (GSK3β) is involved in many pathol. conditions and represents an attractive drug target. We previously reported dual GSK3β/p38α mitogen-activated protein kinase inhibitors and identified N-(4-(4-(4-fluorophenyl)-2-methyl-1H-imidazol-5-yl)pyridin-2-yl)cyclopropanecarboxamide (1) as a potent dual inhibitor of both target kinases. In this study, we aimed to design selective GSK3β inhibitors based on our pyridinylimidazole scaffold. Our efforts resulted in several novel and potent GSK3β inhibitors with IC50 values in the low nanomolar range. 5-(2-(Cyclopropanecarboxamido)pyridin-4-yl)-4-cyclopropyl-1H-imidazole-2-carboxamide (6g) displayed very good kinase selectivity as well as metabolically stability and inhibits GSK3β activity in neuronal SH-SY5Y cells. Interestingly, we observed the importance of the 2-methylimidazole’s tautomeric state for the compound activity. Finally, we reveal how this crucial tautomerism effect is surmounted by imidazole-2-carboxamides, which are able to stabilize the binding via enhanced water network interactions, regardless of their tautomeric state. In the experiment, the researchers used 2-Hydroxyphenylboronic acid(cas: 89466-08-0Recommanded Product: 89466-08-0)
2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Recommanded Product: 89466-08-0
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