One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 497-23-4, Name is Furan-2(5H)-one, formurla is C4H4O2. In a document, author is Szalaj, Natalia, introducing its new discovery. Category: benzofurans.
Multidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer’s disease
Effective therapy of Alzheimer’s disease (AD) requires treatment with a combination of drugs that modulate various pathomechanisms contributing to the disease. In our research, we have focused on the development of multi-target-directed ligands – 5-HT6 receptor antagonists and cholinesterase inhibitors – with disease-modifying properties. We have performed extended in vitro (FRET assay) and in cellulo (Escherichia coli model of protein aggregation) studies on their beta-secretase, tau, and amyloid beta aggregation inhibitory activity. Within these multifunctional ligands, we have identified compound 17 with inhibitory potency against tau and amyloid beta aggregation in in cellulo assay of 59% and 56% at 10 mu M, respectively, hBACE IC50=4 mu M, h5TH6 K (i)=94 nM, hAChE IC50=26 nM, and eqBuChE IC50=5 nM. This study led to the development of multifunctional ligands with a broad range of biological activities crucial not only for the symptomatic but also for the disease-modifying treatment of AD.
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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem