期刊
BIOORGANIC CHEMISTRY
卷 80, 期 -, 页码 43-56出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.05.019
关键词
Organic selenides; Apoptosis; Neurodegeneration; Oligodendrocytes; Multicomponent reactions; Cytoprotective
资金
- Ministere des Affaires Etrangeres: the Embassy of France in Egypt-Institut Francais en Egypte
- Science and Technology Development Fund
- Conseil Regional de Bourgogne (France)
- Ministere de l'Enseignement et de la Recherche (France)
- Egyptian Ministry of Higher Education
- Mansoura University
- COST (European Cooperation in Science and Technology) [CA16112-NutRedOx]
Here a new series of twenty-one organoselenides, of potential protective activity, were synthesized and tested for their intrinsic cytotoxicity, anti-apoptotic and antioxidant capacities in oligodendrocytes. Most of the organoselenides were able to decrease the ROS levels, revealing antioxidant properties. Compounds 5b and 7b showed a high glutathione peroxidase (GPx)-like activities, which were 1.5 folds more active than ebselen. Remarkably, compound 5a diminished the formation of the oligodendrocytes SubG1 peak in a concentration-dependent manner, indicating its anti-apoptotic properties. Furthermore, based on the SwissADME web interface, we performed an in-silico structure-activity relationship to explore the drug-likeness of these organoselenides, predicting the pharmacokinetic parameters for compounds of interest that could cross the blood-brain barrier. Collectively, we present new organoselenide compounds with cytoprotective and antioxidant properties that can be considered as promising drug candidates for myelin diseases.
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