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Dibenzo[1,4,5]thiadiazepine: A hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases

AuthorsGonzález-Muñoz, Gema C. ; Arce, Mariana P. ; Pérez, Concepción; Romero, Alejandro ; Villarroya, Mercedes; López, Manuela G.; Conde, Santiago ; Rodríguez-Franco, María Isabel
Mitochondrial oxidative stress
Calcium modulation
Issue Date2014
CitationEuropean Journal of Medicinal Chemistry 81: 350- 358 (2014)
AbstractIn this work we describe a new family of dibenzo[1,4,5]thiadiazepines (2-12) that showed an interesting in vitro biological profile, namely neuroprotective and antioxidant properties, as well as blockade of cytosolic calcium entry. They showed no cytotoxic effects and the majority were predicted as CNS-permeable compounds. In human neuroblastoma cells they displayed good neuroprotective properties against mitochondrial oxidative stress which, in many cases, almost reached the full protection (>90%) when compounds were incubated with cells 24 h before the addition of toxic stressors. In co-incubation conditions these figures were smaller, although some compounds maintained an interesting level of neuroprotection, higher than 50%. Four selected compounds (2, 5, 8, and 11) were found to be effective antioxidant agents by sequestering mitochondrial radical oxygen species (ROS). Moreover, compound 2 showed a remarkable calcium-channel modulating activity. The interest of these compounds is increased by the fact that dibenzo[1,4,5]thiadiazepine is a barely known structure that is not difficult to synthesize and presents very few described derivatives, opening a new and broad line of research in Medicinal Chemistry. © 2014 Elsevier Inc. All rights reserved.
Identifiersdoi: 10.1016/j.ejmech.2014.04.075
issn: 0223-5234
e-issn: 1768-3254
Appears in Collections:(IQM) Artículos
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