Journal of Medicinal Chemistry · 2018 · 70 citations · 32 references
MedicineMedicinal ChemistryPharmacologyMolecular NeurobiologyMolecular PharmacologyNeuropharmacologyDementia PharmacotherapyEnzyme InhibitionNeurodegenerative Disease PharmacologyNeurodegenerative Disease PharmacotherapyNeuroprotective PharmacologyTau PathologyAlzheimer Disease NeuroprotectionAlzheimer Disease Tau PathologyAnimal Disease ModelsBlood-brain Barrier PermeabilityHistone DeacetylasesNeuroprotective AgentsNeuroprotective MechanismsTau Hyperphosphorylation
value of 3.92 nM. It decreases not only the level of phosphorylation of tau proteins but also the aggregation of tau proteins. Compound 6 also shows neuroprotective activity by triggering ubiquitination. In animal models, compound 6 is able to ameliorate the impaired learning and memory, and it crosses the blood-brain barrier after oral administration. Compound 6 can be developed as a potential treatment for Alzheimer's disease in the future.
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