alpha-synuclein has been researched along with 6-hydroxybenzothiazole* in 1 studies
1 other study(ies) available for alpha-synuclein and 6-hydroxybenzothiazole
| Article | Year |
|---|---|
Discovery of novel 6-hydroxybenzothiazole urea derivatives as dual Dyrk1A/α-synuclein aggregation inhibitors with neuroprotective effects.
A role of Dyrk1A in the progression of Down syndrome-related Alzheimer's disease (AD) is well supported. However, the involvement of Dyrk1A in the pathogenesis of Parkinson's disease (PD) was much less studied, and it is not clear whether it would be promising to test Dyrk1A inhibitors in relevant PD models. Herein, we modified our previously published 1-(6-hydroxybenzo[d]thiazol-2-yl)-3-phenylurea scaffold of Dyrk1A inhibitors to obtain a new series of analogues with higher selectivity for Dyrk1A on the one hand, but also with a novel, additional activity as inhibitors of α-synuclein (α-syn) aggregation, a major pathogenic hallmark of PD. The phenyl acetamide derivative b27 displayed the highest potency against Dyrk1A with an IC Topics: alpha-Synuclein; Cell Survival; Dose-Response Relationship, Drug; Drug Discovery; Dyrk Kinases; HEK293 Cells; Humans; Molecular Structure; Neuroprotective Agents; Protein Aggregates; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Structure-Activity Relationship; Thiazoles; Urea | 2022 |