Abstract
Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.
Highlights
Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities
Sies tested ebselen for its ability to mimic the antioxidant activity of the glutathione peroxidase (GPx) enzyme [2,3], which was recognized as a selenoenzyme few years before [4,5], paving the way for a completely new branch of investigation, the search for strategies and molecules able to cope with oxidative stress [6]
Starting from its synthesis and successive biological evaluation, ebselen can be surely indicated as the most inspiring among the selenorganic compounds. It is currently taken as a reference in several pharmacological investigations even if it is clear that it acts as what medicinal chemists name as a pan-assay interference compound (PAIN) because of its ability to bind non-selectively to reactive cysteines, being nucleophilically attached by the aminoacidic thiol functionality to the electrophilic selenium
Summary
Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Sies tested ebselen for its ability to mimic the antioxidant activity of the glutathione peroxidase (GPx) enzyme [2,3], which was recognized as a selenoenzyme few years before [4,5], paving the way for a completely new branch of investigation, the search for strategies and molecules able to cope with oxidative stress [6]. This selection is devoid of the organic chemistry-oriented papers, which are excluded in PubMed
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