Lewis, Frank W.; Bird, Kathleen; Navarro, Jean-Philippe; El Fallah, Rawa; Brandel, Jeremy; Hubscher-Bruder, Veronique; Tsatsanis, Andrew; Duce, James A.; Tetard, David; Bourne, Samuel; Maina, Mahmoud; Pienaar, Ilse S. published the artcile< Synthesis, physicochemical characterization and neuroprotective evaluation of novel 1-hydroxypyrazin-2(1H)-one iron chelators in an in vitro cell model of Parkinson′s disease>, Recommanded Product: H-Leu-OEt.HCl, the main research area is Parkinson disease iron chelator physicochem property neuroprotective.
Iron dysregulation, dopamine depletion, cellular oxidative stress and α-synuclein protein mis-folding are key neuronal pathol. features seen in the progression of Parkinson′s disease. Iron chelators endowed with one or more therapeutic modes of action have long been suggested as disease modifying therapies for its treatment. In this study, novel 1-hydroxypyrazin-2(1H)-one iron chelators were synthesized and their physicochem. properties, iron chelation abilities, antioxidant capacities and neuroprotective effects in a cell culture model of Parkinson′s disease were evaluated. Physicochem. properties (log β, log D7.4, pL0.5) suggest that these ligands have a poorer ability to penetrate cell membranes and form weaker iron complexes than the closely related 1-hydroxypyridin-2(1H)-ones. Despite this, we show that levels of neuroprotection provided by these ligands against the catecholaminergic neurotoxin 6-hydroxydopamine in vitro were comparable to those seen previously with the 1-hydroxypyridin-2(1H)-ones and the clin. used iron chelator Deferiprone, with two of the ligands restoring cell viability to ≥89% compared to controls. Two of the ligands were endowed with addnl. phenol moieties in an attempt to derive multifunctional chelators with dual iron chelation/antioxidant activity. However, levels of neuroprotection with these ligands were no greater than ligands lacking this moiety, suggesting the neuroprotective properties of these ligands are due primarily to chelation and passivation of intracellular labile iron, preventing the generation of free radicals and reactive oxygen species that otherwise lead to the neuronal cell death seen in Parkinson′s disease.
Dalton Transactions published new progress about Antioxidants. 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Recommanded Product: H-Leu-OEt.HCl.
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