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Closed Access item Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow’s neuroprotective therapies against neurodegenerative diseases
|Authors:||González Muñoz, Gema C.|
Arce, Mariana P.
López, Manuela G
García, Antonio G.
Rodríguez Franco, María Isabel
|Keywords:||Phenothiazines, Dibenzothiadiazepines, Dibenzothiadiazepines, Neuroprotection, Oxidative stress, Butyrylcholinesterase inhibition|
|Citation:||European Journal of Medicinal Chemistry 45 : 6152-6158|
|Abstract:||From an in-house library of compounds, five phenothiazines and one dibenzothiadiazepine were
selected to be tested in neuroprotective and cholinergic assays. Three of them, derived from the
N-alkylphenothiazine, the N-acylaminophenothiazine, and the 1,4,5-dibenzo[b,f]thiadiazepine system,
protected human neuroblastoma cells against oxidative stress generated by both exogenous and mitochondrial
free radicals. They could also penetrate the CNS, according to an in vitro bloodebrain barrier
model, and an N-acylaminophenothiazine derivative behaved as a selective inhibitor of butyrylcholinesterase.
Free radical capture and/or promotion of antioxidant protein biosynthesis are mechanisms
that can be implicated in their neuroprotective actions. Due to their excellent pharmacological
properties and the fact that they were not biologically explored in the past, one N-acylaminophenothiazine
and one 1,4,5-dibenzo[b,f]thiadiazepine have been selected to develop two new series that are
currently in progress|
|Publisher version (URL):||http://dx.doi.org/10.1016/j.ejmech.2010.09.039|
|Appears in Collections:||(IQM) Artículos|
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