| Literature DB >> 29864687 |
Saad Shaaban1, Dominique Vervandier-Fasseur2, Pierre Andreoletti3, Amira Zarrouk4, Philippe Richard2, Amr Negm5, Georg Manolikakes6, Claus Jacob7, Mustapha Cherkaoui-Malki8.
Abstract
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.Entities:
Keywords: Apoptosis; Cytoprotective; Multicomponent reactions; Neurodegeneration; Oligodendrocytes; Organic selenides
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Year: 2018 PMID: 29864687 DOI: 10.1016/j.bioorg.2018.05.019
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275